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523

抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T21343 PTZ-343

PTZ-343 sodium,PTZ 343,吩噻嗪-10-基-丙基磺酸钠盐

Others Others
PTZ-343 是一种鲁米诺的强效发光增强剂 (enhancer)。它极大的增强了过氧化物酶催化的鲁米诺化学发光氧化反应 (>80%) 的光输出。
T10924 Cysteine protease inhibitor-2

Cysteine Protease Proteases/Proteasome
Cysteine protease inhibitor-2 是半胱氨酸蛋白酶抑制剂。
T9693 TBAP-001

Raf MAPK
TBAP-001是RAF 激酶的泛抑制剂,IC50为 62 nM。
T12347 p38-α MAPK-IN-1

p38 MAPK; Autophagy Autophagy; MAPK
p38-α MAPK-IN-1 是一种 MAPK14 (p38-α) 抑制剂,在 EFC 置换试验和 HTRF 试验中 IC50 分别为 2300 nM 和 5500 nM。
T7225 AnaMorelin hydrochloride

RC-1291 hydrochloride,阿拉莫林盐酸盐,ONO-7643 hydrochloride

GHSR GPCR/G Protein
AnaMorelin hydrochloride (RC-1291 hydrochloride) 是生长素受体激动剂,根据 FLIPR 检测,得到 EC50=0.74 nM。
T37591 IMP-1710

DUB Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
IMP-1710 是一种选择性 UCH-L1 抑制剂,在荧光偏振测定中的 IC50 值为 38 nM。
T16727 Relacorilant

CORT 125134

Glucocorticoid Receptor Endocrinology/Hormones
Relacorilant 是一种选择性和口服生物可利用的糖皮质激素受体拮抗剂(HepG2 TAT 试验中的 Kis 为 7.2 nM,在基于细胞的试验中对大鼠、人和猴糖皮质激素受体的 Kis 分别为 12、81.2、210 nM)。 它具有治疗库欣综合征的潜力。
T5410 PD158780

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
PD158780是一种EGFR 家族抑制剂,对EGFR、ErbB2、ErbB3和ErbB4的IC50值分别为8 μM、49、52 和 52 nM。
T8930 CID44216842

KUC103479N-02

CDK; Ras Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
CID44216842 (KUC103479N-02) 是Cdc42选择性抑制剂。在 GDP 结合测定中,它对 Cdc42 野生型和 Cdc42Q61L 突变型的EC50分别为 0.3 和 0.5 μM。在 GTP 结合测定中,它对 Cdc42 野生型和 Cdc42Q61L 突变型的EC50分别为 1.0 和 1.2 μM。它可用作分子探针。
T6935 Nirogacestat

PF-03084014,PF-3084014,PF03084014,PF 03084014

Apoptosis; Gamma-secretase Apoptosis; Neuroscience; Proteases/Proteasome; Stem Cells
Nirogacestat (PF 03084014) 是一种具有口服活性的,可逆的,非竞争性的,选择性γ-secretase 抑制剂,IC50为 6.2 nM。它抑制 Notch 信号通路,可研究 Notch 受体依赖性肿瘤。
T12856 SC-26196

ALPHA,ALPHA-二苯基-4-[(3-吡啶亚甲基)氨基]-1-吡嗪戊腈

Others Others
SC-26196 是一种 Delta6 去饱和酶 (D6D, FADS2) 抑制剂 (在大鼠肝微粒体中,IC50=0.2 µM),具有口服活性,具有抗炎作用。
T12589 PI3Kα/mTOR-IN-1

PI3K; mTOR PI3K/Akt/mTOR signaling
PI3Kα/mTOR-IN-1是一种有效的 PI3Kβ/mTOR 双重抑制剂。在细胞测定中,PI3Kα/mTOR-IN-1的 IC50为7nM,在无细胞测定中 mTOR 和PI3Kβ的Kis 分别为12.5nM 和10.6nM。
T13000 Src Inhibitor 3

Others; Src Angiogenesis; Others; Tyrosine Kinase/Adaptors
Src Inhibitor 3 是一种有效的 c-terminal Src 激酶抑制剂(CSK HTRF 中 IC50 <3 nM,Caliper 中 IC50 <4 nM)。 Src Inhibitor 3 增加由 T 细胞受体信号传导诱导的 T 细胞增殖。
T39785L TH5427

NUDIX hydrolase Metabolism
TH5427 在 NUDT5 活性和 ADP-核糖代谢中有研究的价值。它阻断孕激素依赖性、PAR 衍生的核 ATP 合成以及随后的乳腺癌细胞染色质重塑、基因调控和增殖。NUDT5是乳腺癌细胞激素依赖性基因调控和增殖的变阻器。
T1971 WAY-262611

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
WAY262611是一种 Wnt/β- 联蛋白激动剂,也是一种Dkk1的抑制剂。它能够增加骨形成速率,在 TCF- 荧光素酶测定实验中的EC50=0.63 μM。
T4018 WST-8

WST8

Others Others
WST-8 是水溶性的四唑染料,WTS-8测定法的灵敏度比常规MTS 检测高。
T16115 MLi-2

LRRK2 Autophagy
MLi-2 是一种结构新颖、高效、选择性的 LRRK2 激酶抑制剂,具有中枢神经系统活性,IC50为 0.76 nM,有潜力用于帕金森氏病。
T7904 SR 19881

Estrogen/progestogen Receptor Endocrinology/Hormones
SR 19881 是 ERRγ 的完全激动剂(结合试验中的 EC50 值为 0.39 μM,基于细胞的试验中 EC50 值为 4.7 μM)。
T4988 Boceprevir

SCH 503034,EBP 520,波普瑞韦

HCV Protease; SARS-CoV Microbiology/Virology; Proteases/Proteasome
Boceprevir (SCH 503034) 是一种口服有效的选择性 HCV NS3 蛋白酶抑制剂。在酶试验中的 Ki 为 14 nM,在基于细胞的复制子试验中 EC90 为 350 nM。它也是 SARS-CoV-2 3CLpro 抑制剂。
T20490 Z-Arg(Z)2-OH

NSC120011,NSC-120011,NSC 120011,Tris(benzyloxycarbonyl)arginine

Others Others
Z-Arg(Z)2-OH 可用于检测螨匀浆中的蛋白水解活性的实验中。
T9322 N-Phenylacrylamide

Others Others
N-Phenylacrylamide 通过荧光转酰胺法抑制人重组 TGM2。
T4470 Pyridostatin TFA

DNA/RNA Synthesis Cell Cycle/Checkpoint; DNA Damage/DNA Repair
Pyridostatin TFA 是一种 G-四链体稳定剂,靶向原癌基因 Src,降低人乳腺癌细胞 SRC 蛋白水平和 SRC 依赖的细胞运动。它通过诱导复制和转录依赖的 DNA 损伤促进人类癌细胞生长停滞。
T12128 Mutant IDH1-IN-2

Isocitrate Dehydrogenase (IDH) Metabolism
Mutant IDH1-IN-2是突变型异柠檬酸脱氢酶蛋白抑制剂, 在荧光生物化学检测中IC50为16.6 nM,LS-MS 生物化学检测中IC50为<22 nM,。
T6868 KYA1797K

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
KYA1797K 是一种选择性 Wnt/β-catenin 抑制剂(IC50:0.75 µM)。
T8765 iGOT1-01

Others Others
iGOT1-01 是一种天冬氨酸转氨酶 1 (谷氨酸草酰乙酸转氨酶 1;GOT1) 抑制剂,在 GOT1/GLOX/HRP 测定中IC50为 11.3 μM,在 MDH 偶联 GOT1 酶法测定中IC50为 85 μM。它显示出抗癌活性。
T9681 MAK-683 hydrochloride

Histone Methyltransferase Chromatin/Epigenetic
MAK683 hydrochloride 是胚胎外胚层发育 (EED) 抑制剂。MAK683 hydrochloride 在 EED Alphascreen, ELISA 和 LC-MS 试验中测得的IC50 值分别为 59,26,89 nM。
T9994 WAY-620521

Others Others
WAY-620521是一种用于细胞的高通量测定小分子。
T4219 Autophinib

PI3K; Autophagy Autophagy; PI3K/Akt/mTOR signaling
Autophinib 是一种选择性细胞自噬抑制剂,通过靶向 VPS34来抑制饥饿或雷帕霉素诱导的细胞自噬,对于饥饿和雷帕霉素诱导的自噬,IC50值分别为 90 nM 和 40 nM。它还是 ATP 竞争性 VPS34抑制剂,其 IC50值为 19 nM。
T9448 IL-17A inhibitor 1

IL Receptor Immunology/Inflammation
IL-17A inhibitor 1 是 IL-17A 的抑制剂,在alphalisa assay 中的IC50为 <9.45 nM。IL-17A inhibitor 1抑制HT-29 细胞的 IC50 值为 9.3 nM。
T18997 GPDA

Glycylproline p-nitroanilide tosylate,GPN

Others Others
GPDA (Glycylproline p-nitroanilide tosylate) 是一种酶促反应检测底物,用于检测脯氨酰二肽氨基肽酶。
T4390 ML221

Apelin receptor; Arrestin GPCR/G Protein
ML221 是apelin (APJ)拮抗剂,能够抑制 apelin-13 介导的 APJ 的活化,在 cAMP 试验和 β-arrestin 实验中,IC50值分别为 0.70 μM 和 1.75 μM,EC80值均为 10 nM。
T17203 UNC0224

Histone Methyltransferase Chromatin/Epigenetic
UNC0224 是 G9a 的特异性抑制剂,Ki 为 2.6 nM,IC50 为 15 nM。 UNC0224 还有效抑制 GLP,IC50 值为 20-58 nM。
T11561 HIF-2α-IN-2

HIF/HIF Prolyl-Hydroxylase; HIF Angiogenesis; Chromatin/Epigenetic; Metabolism
HIF-2α-IN-2 是低氧诱导因子抑制剂,IC50=16 nM。
T10319 Anamorelin

RC-1291,阿拉莫林,ONO-7643

GHSR GPCR/G Protein
Anamorelin (ONO-7643) 是新型ghrelin receptor 激动剂,根据FLIPR 检测,得到其EC50=0.74 nM。
T1989 Luminespib

AUY922,VER-52296,NVP-AUY922

Apoptosis; HSP; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling; Metabolism
Luminespib (VER-52296) 是一种 HSP90抑制剂,抑制 HSP90α 和 HSP90β 的 IC50分别为 7.8 和 21 nM。
T15665 KJ Pyr 9

c-Myc; Autophagy Autophagy; Cell Cycle/Checkpoint
KJ Pyr 9 是一种 MYC 的抑制剂,在体外实验中的 Kd 值为 6.5 nM。
T2001 PF-573228

PF 573228

Apoptosis; FAK Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
PF-573228是一种选择性的 FAK 抑制剂,对 FAK 纯化重组催化片段的 IC50值为4 nM。
T36711 FM19G11

FM19G11,HIF-1alpha/2alpha Inhibitor

HIF Angiogenesis; Chromatin/Epigenetic
FM19G11 是一种低氧诱导因子 (HIF) α-亚基抑制剂(在低氧诱导的荧光素酶试验中 IC50 为 80 nM)。
T9969 EZM0414

Histone Methyltransferase Chromatin/Epigenetic
EZM0414 是一种有效、选择性、口服生物利用度高的SETD2抑制剂,在 SETD2 生化分析中,IC50值为18 nM;在细胞分析中,IC50值为34 nM。EZM0414可用于复发或难治性多发性骨髓瘤和弥漫性大 B 细胞淋巴瘤的研究。
T2508 Binimetinib

ARRY-438162,ARRY-162,MEK162

MEK; Autophagy Autophagy; MAPK
Binimetinib (ARRY-162) 是一种可口服的选择性 MEK1/2抑制剂,抑制MEK 的IC50为 12 nM。
T3198L PRE-084 hydrochloride

Sigma receptor GPCR/G Protein
PRE-084 hydrochloride 是 σ1 的选择性激动剂在sigma 受体检测中,IC50值为44 nM。
T0238 2-(Acetyloxy)-3-Methylbenzoic Acid

Others Others
2-(Acetyloxy)-3-Methylbenzoic Acid 用于 qHTS 测定羟基类固醇 (17-β) 脱氢酶 4、HSD17B4 的抑制剂,活性值为 19.95 μM。
T15201 MAK683

Histone Methyltransferase Chromatin/Epigenetic
MAK683 是胚胎外胚层发育 (EED) 抑制剂。在 EED Alphascreen 结合、LC-MS 和 ELISA 测定中,IC50值为 59、89 和 26 nM。
T8959 OS-3-106

Dopamine Receptor GPCR/G Protein; Neuroscience
OS-3-106 是一种新型芳酰胺苯基哌嗪,在腺苷酸环化酶抑制试验中作为 D3R 的部分激动剂。
T2654 GSK2656157

Apoptosis; PERK; Autophagy Apoptosis; Autophagy
GSK2656157 是一种ATP 竞争性的PERK 选择性抑制剂,IC50值为 0.9 nM。
T2380 BIBR 1532

Apoptosis; Telomerase Apoptosis; DNA Damage/DNA Repair
BIBR 1532 是一种选择性端粒酶非竞争性抑制剂,IC50值为 100 nM。
T14371 Barasertib

巴拉塞替,AZD1152

Apoptosis; Aurora Kinase Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic
Barasertib (AZD1152) 是 Barasertib-hQPA 的前体药物,在癌细胞中诱导生长停滞和凋亡。它是高度选择性的Aurora B 抑制剂,IC50值为 0.37 nM。
T2452 C646

Apoptosis; Epigenetic Reader Domain; Histone Acetyltransferase; Autophagy Apoptosis; Autophagy; Chromatin/Epigenetic
C646 是一种竞争性组蛋白乙酰转移酶 p300选择性抑制剂,Ki 值为 400 nM,对其他乙酰转移酶作用较小。
T6070 (E/Z)-Rigosertib sodium

N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐,(E/Z) ON-01910 sodium

PLK Cell Cycle/Checkpoint
ON-01910 是一种非 ATP 竞争性 PLK1 抑制剂(IC50 为 9 nM,在无细胞试验中)。它对 Plk2 的选择性高出 30 倍,对 Plk3 没有活性。 Rigosertib 抑制 PI3K/Akt 通路并激活氧化应激信号。 Rigosertib 可诱导多种癌细胞凋亡。它是一种合成的苄基苯乙烯基砜类似物,具有潜在的抗肿瘤活性。
T13214L TRPV4 agonist-1 free base

OUN67600

TRP/TRPV Channel Membrane transporter/Ion channel
TRPV4 agonist-1 free base (OUN67600) 是有效的瞬时受体电位香草酸亚型 4 激动剂, hTRPV4 Ca2+实验中 EC50值为60 nM。

化合物

PTZ-343
Cat.No: T21343
Synonym: PTZ-343 sodium,PTZ 343,吩噻嗪-10-基-丙基磺酸钠盐
Target: Others
Cysteine protease inhibitor-2
Cat.No: T10924
Synonym:
Target: Cysteine Protease
TBAP-001
Cat.No: T9693
Synonym:
Target: Raf
p38-α MAPK-IN-1
Cat.No: T12347
Synonym:
Target: p38 MAPK, Autophagy
AnaMorelin hydrochloride
Cat.No: T7225
Synonym: RC-1291 hydrochloride,阿拉莫林盐酸盐,ONO-7643 hydrochloride
Target: GHSR
IMP-1710
Cat.No: T37591
Synonym:
Target: DUB
Relacorilant
Cat.No: T16727
Synonym: CORT 125134
Target: Glucocorticoid Receptor
PD158780
Cat.No: T5410
Synonym:
Target: EGFR
CID44216842
Cat.No: T8930
Synonym: KUC103479N-02
Target: CDK, Ras
Nirogacestat
Cat.No: T6935
Synonym: PF-03084014,PF-3084014,PF03084014,PF 03084014
Target: Apoptosis, Gamma-secretase
SC-26196
Cat.No: T12856
Synonym: ALPHA,ALPHA-二苯基-4-[(3-吡啶亚甲基)氨基]-1-吡嗪戊腈
Target: Others
PI3Kα/mTOR-IN-1
Cat.No: T12589
Synonym:
Target: PI3K, mTOR
Src Inhibitor 3
Cat.No: T13000
Synonym:
Target: Others, Src
TH5427
Cat.No: T39785L
Synonym:
Target: NUDIX hydrolase
WAY-262611
Cat.No: T1971
Synonym:
Target: Wnt/beta-catenin
WST-8
Cat.No: T4018
Synonym: WST8
Target: Others
MLi-2
Cat.No: T16115
Synonym:
Target: LRRK2
SR 19881
Cat.No: T7904
Synonym:
Target: Estrogen/progestogen Receptor
Boceprevir
Cat.No: T4988
Synonym: SCH 503034,EBP 520,波普瑞韦
Target: HCV Protease, SARS-CoV
Z-Arg(Z)2-OH
Cat.No: T20490
Synonym: NSC120011,NSC-120011,NSC 120011,Tris(benzyloxycarbonyl)arginine
Target: Others
N-Phenylacrylamide
Cat.No: T9322
Synonym:
Target: Others
Pyridostatin TFA
Cat.No: T4470
Synonym:
Target: DNA/RNA Synthesis
Mutant IDH1-IN-2
Cat.No: T12128
Synonym:
Target: Isocitrate Dehydrogenase (IDH)
KYA1797K
Cat.No: T6868
Synonym:
Target: Wnt/beta-catenin
iGOT1-01
Cat.No: T8765
Synonym:
Target: Others
MAK-683 hydrochloride
Cat.No: T9681
Synonym:
Target: Histone Methyltransferase
WAY-620521
Cat.No: T9994
Synonym:
Target: Others
Autophinib
Cat.No: T4219
Synonym:
Target: PI3K, Autophagy
IL-17A inhibitor 1
Cat.No: T9448
Synonym:
Target: IL Receptor
GPDA
Cat.No: T18997
Synonym: Glycylproline p-nitroanilide tosylate,GPN
Target: Others
ML221
Cat.No: T4390
Synonym:
Target: Apelin receptor, Arrestin
UNC0224
Cat.No: T17203
Synonym:
Target: Histone Methyltransferase
HIF-2α-IN-2
Cat.No: T11561
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase, HIF
Anamorelin
Cat.No: T10319
Synonym: RC-1291,阿拉莫林,ONO-7643
Target: GHSR
Luminespib
Cat.No: T1989
Synonym: AUY922,VER-52296,NVP-AUY922
Target: Apoptosis, HSP, Autophagy
KJ Pyr 9
Cat.No: T15665
Synonym:
Target: c-Myc, Autophagy
PF-573228
Cat.No: T2001
Synonym: PF 573228
Target: Apoptosis, FAK
FM19G11
Cat.No: T36711
Synonym: FM19G11,HIF-1alpha/2alpha Inhibitor
Target: HIF
EZM0414
Cat.No: T9969
Synonym:
Target: Histone Methyltransferase
Binimetinib
Cat.No: T2508
Synonym: ARRY-438162,ARRY-162,MEK162
Target: MEK, Autophagy
PRE-084 hydrochloride
Cat.No: T3198L
Synonym:
Target: Sigma receptor
2-(Acetyloxy)-3-Methylbenzoic Acid
Cat.No: T0238
Synonym:
Target: Others
MAK683
Cat.No: T15201
Synonym:
Target: Histone Methyltransferase
OS-3-106
Cat.No: T8959
Synonym:
Target: Dopamine Receptor
GSK2656157
Cat.No: T2654
Synonym:
Target: Apoptosis, PERK, Autophagy
BIBR 1532
Cat.No: T2380
Synonym:
Target: Apoptosis, Telomerase
Barasertib
Cat.No: T14371
Synonym: 巴拉塞替,AZD1152
Target: Apoptosis, Aurora Kinase
C646
Cat.No: T2452
Synonym:
Target: Apoptosis, Epigenetic Reader Domain, Histone Acetyltransferase, Autophagy
(E/Z)-Rigosertib sodium
Cat.No: T6070
Synonym: N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐,(E/Z) ON-01910 sodium
Target: PLK
TRPV4 agonist-1 free base
Cat.No: T13214L
Synonym: OUN67600
Target: TRP/TRPV Channel
Cat. No. Product Name Target Signaling Pathways
TN3112 5-Heneicosylresorcinol

NADPH-oxidase; Antifection Immunology/Inflammation; Microbiology/Virology
5-Heneicosylresorcinol 对 RBL-2H3 细胞中 β-己糖胺酶的释放具有抑制作用,它还可以防止 3T3-L1 细胞中甘油三酯的积累。它对红线虫、秀丽隐杆线虫和松材线虫具有杀线虫活性,ED50 值分别为 80、30 和 180 ug/mL。
T4086 Glycyl-L-leucine

甘氨酰-L-亮氨酸,Gly-Leu

Others Others
Glycyl-L-leucine (Gly-Leu) 是一种可用作糖基亮氨酸二肽酶底物的二肽。
T2814 Cryptotanshinone

隐丹参酮,Cryptotanshinon,Tanshinone c,隐丹参醌

STAT; Autophagy Autophagy; JAK/STAT signaling; Stem Cells
Cryptotanshinone (Cryptotanshinon) 是从丹参的根中提取的一种天然产物,抑制STAT3的IC50为4.6 μM,具有抗肿瘤活性。
T5S1550 Cinnamyl alcohol

肉桂醇,肉桂醇;beta-苯丙烯醇,Cinnamic Alcohol,Styryl Carbinol

PPAR DNA Damage/DNA Repair; Metabolism
Cinnamyl alcohol (Styryl Carbinol) 是从板栗花中分离得到的一种活性成分,抑制增加的 PPARγ表达,具有抗肥胖作用。
TN1112 Morellic acid

Others Others
Morellic acid 提取于 Garcinia Morella 中,具有抗血管生成作用。
T4S0176 Alnustone

(4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one,桤木酮

Others Others
Alnustone ((4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one) 是一种非酚双苯庚烷类化合物,在草药和香料中发现,是姜黄的成分之一,具有抗吐、抗炎作用。
TN1691 Glabrol

光甘草酚,光甘草醇

P450; NF-κB; NO Synthase; Acyltransferase Immunology/Inflammation; Metabolism; NF-κB
Glabrol 是分离自甘草根的乙醇提取物中的一种异戊二烯类黄酮,是一种有效且非竞争性的酰基辅酶 A:胆固醇酰基转移酶(ACAT)抑制剂,抑制大鼠肝脏微粒体 ACAT 的 IC50为 24.6 μM。
TN2030 P-Hydroxyphenethyl trans-ferulate

反式-阿魏酸对羟基苯乙酯

5-HT Receptor GPCR/G Protein; Neuroscience
p-Hydroxyphenethyl trans-ferulate 具有抗高血糖 (酵母α-葡萄糖苷酶,IC5019.24 ± 1.73 µmol L-1),抗氧化,抗炎活性,也具有抗癌特性和血清素能特性。
T36473 trans-Nerolidol

trans-Nerolidol is a sesquiterpene that has been found in various plants, includingC. sativa, and has diverse biological activities, including antimicrobial, antioxidant, anticancer, and insecticidal properties.1,2,3,4In a disc assay,trans-nerolidol inhibits the growth ofS. aureus,B. subtilis,E. coli, andS. cerevisiaewith zones of inhibition measuring 10, 9, 10, and 4 mm, respectively.2It reduces viability of CaCo-2 adenocarcinoma cells with an IC50value of 28.7 mg/L and reduces production of re...
T5853 Rubitecan

RFS 2000,鲁比特康,9-Nitrocamptothecin

Topoisomerase DNA Damage/DNA Repair
Rubitecan (9-Nitrocamptothecin) 是一种与喜树碱相关的半合成药物,具有有效的抗肿瘤和抗病毒特性。它是一种 DNA 拓扑异构酶 I 抑制剂,以浓度依赖性方式抑制 DNA 拓扑异构酶 I 并在无细胞试验中增加超螺旋 DNA 的比例。
TN2086 Piperlotine A

Antibacterial Microbiology/Virology
Piperlotine A 是一种可从罗洛胡椒中提取得到的生物碱,具有抗血小板聚集活性。Piperlotine A 在体外试验中显示出对结核分枝杆菌的抑制作用,MIC 值为 50 ug/mL。
T36914 2-Hydroxyanthraquinone

Others Others
2-Hydroxyanthraquinone 是一种天然产物,显示出抗肿瘤和免疫抑制活性。
T35749 Thymohydroquinone

Thymoquinol

Antioxidant; Reactive Oxygen Species Immunology/Inflammation; Metabolism; NF-κB; oxidation-reduction
Thymohydroquinone (Thymoquinol) 是中药材百里香、牛至和其他唇形科植物中含有的单萜酚类化合物。 Thymohydroquinone 抑制癌细胞生长、减少氧化应激和调节炎症反应,在无细胞实验中清除2,2-二苯基-1-picrylhydrazyl 自由基(IC50 = 2.4 μg/ml),在浓度为1.6至6.4 μg/ml 的氧自由基吸收能力(ORAC)实验中,它的Trolox 当量值为2.6胸腺对苯二酚对A2780、OVCAR-8和CIS-A2780卵巢癌细胞(IC50分别为3.1、8.9和9.8 μM)和人卵巢永生化上皮细胞(IC50 = 14 μM)的生长有抑制作用,体外对恶性疟原虫也有抑制作用(IC50 = 15.9 μM)。
T1737 Genistein

NPI 031L,三叶草,染料木素,金雀异黄酮

Apoptosis; EGFR; Endogenous Metabolite; Autophagy Angiogenesis; Apoptosis; Autophagy; JAK/STAT signaling; Metabolism; Tyrosine Kinase/Adaptors
Genistein (NPI 031L) 是一种大豆异黄酮,是一种多重的酪氨酸激酶抑制剂,通过改变细胞凋亡,细胞周期和血管生成以及抑制转移对多种癌症有化疗作用。
T37753 Aureusimine B

Cysteine Protease; Antibacterial Microbiology/Virology; Proteases/Proteasome
Aureusimine B 是一种钙蛋白酶抑制剂,由金黄色葡萄球菌生物膜产生,可能是金黄色葡萄球菌生物膜感染的潜在生物标志物。
TN6657 4-(Dimethylamino)cinnamaldehyde

4-Dimethylaminocinnamaldehyde is a photometric reagent for primary aromatic amines. The 4-(dimethylamino)cinnamaldehyde assay is currently used to quantify proanthocyanidin (PAC) content in cranberry products.
T82640 Cyclobisdemethoxycurcumin

Cyclobisdemethoxycurcumin,作为一种抗氧化剂,在DPPH自由基清除试验中示出约250 μM的IC50,在2-DR氧化试验中显示为15-20 μM的IC50。
TMA0245 Hexacosyl (E)-ferulate

Others Others
Hexacosyl (E)-ferulate displays significant antioxidant activity in the DPPH assay (RC50 = 0.0976 mg/mL). It also might be a chemotaxonomic marker in the genus Echinops.
TMA2563 Pedalitin

Tyrosinase Proteases/Proteasome
Pedalitin is a mixed-type inhibitor of tyrosinase. In the assay of α-glucosidase inhibition, rosmarinic acid is a competitive inhibitor, whereas both methyl rosmarinate and Pedalitin are mixed-type inhibitors.
TN1802 Isoscoparin-2′′O-glucoside

异金雀花素-2”-O-吡喃葡萄糖苷,Isoscoparin-2''-Beta-D-glucopyranoside

Others Others
Isoscoparin-2''-Beta-D-glucopyranoside shows prominent free radical scavenging activity in DPPH assay.
TN4602 Myricananin A

NOS Immunology/Inflammation
Myricadenin A exhibits anti-inflammatory activities in the iNOS assay with EC50 values of 18.1 uM.
TN3705 Coronalolide methyl ester

HIV Protease Microbiology/Virology; Proteases/Proteasome
Coronalolide methyl ester displays significant anti-HIV activities in the HIV-1RT assay. It and coronalolide show broad cytotoxic activity against a panel of human cancer cell lines.
T36044 17-hydroxy Venturicidin A

17-hydroxy Venturicidin A is a macrolide fungal metabolite originally isolated from Streptomyces. It has antibiotic activity against M. luteus, B. subtilis, and S. aureus and antifungal activity against V. dahlia, Fusarium, and C. tropicalis in a disc assay.
T13679 Enniatin B

ERK MAPK
Enniatins B decreases the activation of ERK (p44/p42). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes.
TN2834 27-p-Coumaroyloxyursolic acid

Others Others
27-trans-p-Coumaroyloxyursolic acid and 27-cis-p-coumaroyloxyursolic acid show potent inhibitory activity in the acyl CoA cholesteryl acyl transferase (ACAT) assay.
T83467 10-O-Trans-p-methoxycinnamoylcatalpol

10-O-Trans-p-methoxycinnamoylcatalpol 表现出抗氧化特性,DPPH 自由基清除实验中显示其 IC50 为 0.37 μM/mL。
TN3921 Effusanin B

Antifection Microbiology/Virology
Effusanin B shows antibacterial activity. It exhibits DNA-damaging activity in assay which employes DNA-repair deficient (RAD 52Y) and repair proficient (RAD +) yeast strains.
T38349 Talaromycesone A

Talaromycesone A is a fungal metabolite originally isolated fromTalaromyces.1It is active againstS. epidermidisand methicillin-resistantS. aureus(MRSA) bacteria (IC50s = 3.70 and 5.48 μM, respectively). Talaromycesone A inhibits acetylcholinesterase (AChE) in a cell-free assay (IC50= 7.49 μM for the human enzyme). 1.Wu, B., Ohlendorf, B., Oesker, V., et al.Acetylcholinesterase inhibitors from a marine fungus Talaromyces sp. strain LF458Mar. Biotechnol. (NY)17(1)110-119(2015)
TN1265 3'-O-Methylorobol

3'-O-METHYLOROBOL,3'-O-甲基香豌豆苷元

Others Others
3'-O-Methylorobol exhibits moderate antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay, it also exerts potential analgesic properties. 3'-O-Methylorobol can increase osteoblast differentiation.
TN4342 Izalpinine

Others Others
Izalpinin exhibits potent antioxidant activities in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay. Izalpinin exhibits inhibitory role of muscarinic receptor-related detrusor contractile activity, and it may be a promising lead compound to treat overactiv
T37543 Anhydroepiophiobolin A

Anhydroepiophiobolin A is a sesterterpenoid fungal metabolite that has been found in B. oryzae. It is cytotoxic to HepG2 and K562 cells (IC50s = 47.1 and 35.6 μM, respectively) as well as A549, SKOV3, SK-MEL-2, XF498, and HCT15 cells (IC50s = 1.6-1.9 μg/ml). Anhydroepiophiobolin A is phytotoxic to S. viridis and D. erucoides in a leaf puncture assay.
T38104 Deoxyfusapyrone

Deoxyfusapyrone is an α-pyrone fungal metabolite originally isolated from F. semitectum and has antifungal activity. It is active against C. neoformans, A. fumigatus, A. niger, and A. flavus human mycoses (MICs = 1.56-6.25 μg/ml). Deoxyfusapyrone is also active against a variety of filamentous fungi, but not yeast or the bacterium B. megaterium, in a disc assay.
TN3704 Coronalolide

HIV Protease Microbiology/Virology; Proteases/Proteasome
Coronalolide shows significant cytotoxic activities in P-388 cell line, it also displays significant anti-HIV activities in the HIV-1RT assay. Coronalolide and coronalolide methyl ester show broad cytotoxic activity against a panel of human cancer cell li
T36513 Pyranonigrin A

Pyranonigrin A is a fungal metabolite originally isolated from Aspergillus that has antioxidant activity. It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH;) free radicals in a cell-free assay (IC50 = 132.9 μM). Pyranonigrin A (10 μM) suppresses TNF-α-induced expression of vascular cell adhesion molecule 1 (VCAM-1) in human umbilical vein endothelial cells (HUVECs).
TN5133 3',5,5',7-Tetrahydroxy-4',6-dimethoxyflavone

HIV Protease; Topoisomerase DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
5,7,3',5'-tetrahydroxy-6,4'-dimethoxyflavone exhibits anti-HIV-1 activity in the anti-syncytium assay using (∆Tat/rev)MC99 virus and 1A2 cell line system, it shows considerably activity against HIV-1 reverse transcriptase. It exhibits cytotoxic activity against P-388 cell lines, it can inhibit DNA topoisomerase IIα activity, which may be responsible for the observed cytotoxicity.
T83578 (19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol

(19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol 是一种葫芦烷型三萜。该化合物在 MTT 法检测中对癌细胞系 MCF-7、HepG2、Du145、Colon205 以及 HL-60 均未表现出抑制效果。
TN3920 Effusanin A

Raf; Antifection MAPK; Microbiology/Virology
Effusanin A 是一种存在于Isodon rugosus 之中的天然产物。 它具有 DNA 损伤和抗菌作用。
TN5880 Mesuol

Mesuol has antioxidant activity, it shows very high scavenging activity against DPPH radical; it also has immunomodulatory activity, can potentiate percentage neutrophil adhesion in neutrophil adhesion test in rats and phagocytosis in carbon clearance assay. Mesuol can suppress HIV-1 replication in Jurkat T cells, it inhibits TNFα-induced HIV-1-LTR transcriptional activity by targeting the nuclear factor-κB (NF-κB) pathway.
T38015 Herquline A

Herquline A is an alkaloid fungal metabolite originally isolated from P. herquei. It inhibits cell death induced by influenza A strain A/PR/8/34 in MDCK cells with an IC50 value of 10 μg/ml and inhibits viral replication in a plaque assay in a concentration-dependent manner. Herquline A also inhibits platelet aggregation induced by ADP and platelet-activating factor (PAF) in vitro (IC50s = 180 and 240 μM, respectively).
TN4113 Garcinone E

Antifection Microbiology/Virology
Garcinone E is active constituents in the anticomplement assay used. Garcinone E exhibits potent activity in vitro against Plasmodium falciparum chloroquine-resistant strain W2, with IC50 values below 3 µM. It has potent cytotoxic effect on all hepatocellular carcinomas cell lines as well as on the other gastric and lung cancer cell lines included in the screen, may be potentially useful for the treatment of certain types of cancer.
T35609 19-O-Acetylchaetoglobosin A

19-O-Acetylchaetoglobosin A is a fungal metabolite originally isolated fromC. globosumthat has actin polymerization inhibitory and cytotoxic activities.1,2It inhibits actin polymerization in a cell-free assay when used at a concentration of 2 μM.219-O-Acetylchaetoglobosin A (3.2, 10, and 32 μg/ml) is cytotoxic to HeLa cervical cancer cells.1 1.Umeda, M., Ohtsubo, K., Saito, M., et al.Cytotoxicity of new cytochalasans from Chaetomium globosumExperientia31(4)435-438(1975) 2.Sekita, S., Yoshihira, ...
T83913 Mitraciliatine

Mitraciliatine是一种在M. speciosa(泰国称为Kratom)中发现的生物碱,是μ-阿片受体(MOR)部分激动剂和κ-阿片受体(KOR)激动剂。该化合物对MOR和KOR具有选择性,与δ-阿片受体(DOR; EC50s分别为228, 218, 和 >1,000 nM,针对小鼠受体在GTPγS结合实验中的表现)。Mitraciliatine(100 nmol/动物,脑室内注射)在小鼠的热水尾部缩回实验中延长了撤回潜伏期,这一效果可以通过敲除MOR而非KOR来逆转。与吗啡不同,Mitraciliatine不会诱发过度活动或呼吸抑制。
T36815 Chevalone C

Chevalone C is a meroterpenoid fungal metabolite originally isolated from E. chevalieri. It is active against M. tuberculosis H37Ra (MIC = 6.3 μg/ml) and is cytotoxic to BC1 human breast cancer cells (IC50 = 8.7 μg/ml). Chevalone C inhibits the growth of multidrug-resistant isolates of E. coli, S. aureus, and E. faecium in a disc diffusion assay when used at a concentration of 15 μg/disc. It also induces cell death in HCT116 colorectal carcinoma cells.
T33492 Methyl pyropheophorbide-a

MPPa (Methyl pyropheophorbide-a),NSC267052,Pyropheophorbidea,MPPa,NSC-267052,NSC 267052

Pyropheophorbide-a methyl ester (MPPa) is a PDT photosensitizer, and is also a semisynthetic natural product derived from chlorophyll a. The absorption peak of MPPa in organic solvent and in cells was at 667 and 674 nm, respectively. 3-(4,5-Dimethylthiazo
T38097 Antibiotic PF 1052

Antibiotic PF 1052 is a fungal metabolite originally isolated from Phoma.1,2 It is active against S. aureus, S. parvulus, and C. perfringens (MICs = 3.13, 0.78, and 0.39 μg/ml, respectively), among others.1 It inhibits neutrophil migration in a wound assay using zebrafish larvae expressing GFP-labeled neutrophils, reducing pseudopodia formation and inducing rounding of neutrophils.2 Antibiotic PF 1052 is selective for neutrophil migration over macrophage migration in zebrafish larvae. It also in...
T79965 11-Oxoisomogroside V

Metabolism
11-Oxoisomogroside V(compound 3)是从罗汉果粗提物中分离的一种葫芦苷,能够激活PGC-1α的转录活性。荧光素酶实验表明,10 μM 和 20 μM 浓度的11-Oxoisomogroside V分别将荧光素酶活性提高至 133.79% 和 143.81%。
TN5655 Broussonin B

Broussonins A and B, new phytoalexins from diseased paper mulberry. Broussonin B can induce neurite outgrowth in PC-12 cells at concentration of 50 microg/ml, and show moderate inhibitory activities against a chymotrypsin-like activity of the proteasome.B
T36992 Monocerin

Monocerin is a fungal metabolite that has been found inF. larvarumand has diverse biological activities.1,2,3It is active against the bacteriaE. coliandB. megaterium, the phytopathogenic fungusM. violaceum, and the algaC. fuscain an agar diffusion assay when used at a concentration of 50 μg/disc.1Monocerin (17.5 μg/ml) induces mortality in adultC. erythrocephala.2It reduces root elongation in pre-germinatedS. halepenseseeds when used at a concentration of 33 ppm.3 1.Zhang, W., Krohn, K., Draeger...
T37714 Fuscin

Fuscin is a quinonoid fungal metabolite originally isolated from O. fuscum that has diverse biological activities. It inhibits binding of the ADP/ATP translocase inhibitor atractyloside to rat liver mitochondria in an ADP-dependent manner when used at a concentration of 50 μM in a radioligand binding assay. Fuscin (20 μM) reduces the glutathione content of rat liver mitochondria to 28% of controls and inhibits NADH oxidation in sonicated pigeon heart mitochondria preparations in a concentration-...
T36438 Sporogen-AO 1

Sporogen-AO 1 is a fungal metabolite originally isolated fromA. oryzaethat has diverse biological activities.1,2,3,4,5It inhibits HIV-1 Tat transactivation in a cell-based assay with an IC50value of 15.8 μM.4Sporogen-AO 1 is cytotoxic to HeLa, KB, and NCI H187 cancer cells (IC50s = 8.3, 9, and 5.1 μM, respectively).2,5It is active againstC. albicans(MIC = 4 mM).3 1.Tanaka, S., Wada, K., Marumo, S., et al.Structure of sporogen-ao 1, a sporogenic substance of Aspergillus oryzaeTetrahedron Lett.25(...
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天然产物

5-Heneicosylresorcinol
Cat.No: TN3112
Synonym:
Target: NADPH-oxidase, Antifection
Glycyl-L-leucine
Cat.No: T4086
Synonym: 甘氨酰-L-亮氨酸,Gly-Leu
Target: Others
Cryptotanshinone
Cat.No: T2814
Synonym: 隐丹参酮,Cryptotanshinon,Tanshinone c,隐丹参醌
Target: STAT, Autophagy
Cinnamyl alcohol
Cat.No: T5S1550
Synonym: 肉桂醇,肉桂醇;beta-苯丙烯醇,Cinnamic Alcohol,Styryl Carbinol
Target: PPAR
Morellic acid
Cat.No: TN1112
Synonym:
Target: Others
Alnustone
Cat.No: T4S0176
Synonym: (4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one,桤木酮
Target: Others
Glabrol
Cat.No: TN1691
Synonym: 光甘草酚,光甘草醇
Target: P450, NF-κB, NO Synthase, Acyltransferase
P-Hydroxyphenethyl trans-ferulate
Cat.No: TN2030
Synonym: 反式-阿魏酸对羟基苯乙酯
Target: 5-HT Receptor
trans-Nerolidol
Cat.No: T36473
Synonym:
Target:
Rubitecan
Cat.No: T5853
Synonym: RFS 2000,鲁比特康,9-Nitrocamptothecin
Target: Topoisomerase
Piperlotine A
Cat.No: TN2086
Synonym:
Target: Antibacterial
2-Hydroxyanthraquinone
Cat.No: T36914
Synonym:
Target: Others
Thymohydroquinone
Cat.No: T35749
Synonym: Thymoquinol
Target: Antioxidant, Reactive Oxygen Species
Genistein
Cat.No: T1737
Synonym: NPI 031L,三叶草,染料木素,金雀异黄酮
Target: Apoptosis, EGFR, Endogenous Metabolite, Autophagy
Aureusimine B
Cat.No: T37753
Synonym:
Target: Cysteine Protease, Antibacterial
4-(Dimethylamino)cinnamaldehyde
Cat.No: TN6657
Synonym:
Target:
Cyclobisdemethoxycurcumin
Cat.No: T82640
Synonym:
Target:
Hexacosyl (E)-ferulate
Cat.No: TMA0245
Synonym:
Target: Others
Pedalitin
Cat.No: TMA2563
Synonym:
Target: Tyrosinase
Isoscoparin-2′′O-glucoside
Cat.No: TN1802
Synonym: 异金雀花素-2”-O-吡喃葡萄糖苷,Isoscoparin-2''-Beta-D-glucopyranoside
Target: Others
Myricananin A
Cat.No: TN4602
Synonym:
Target: NOS
Coronalolide methyl ester
Cat.No: TN3705
Synonym:
Target: HIV Protease
17-hydroxy Venturicidin A
Cat.No: T36044
Synonym:
Target:
Enniatin B
Cat.No: T13679
Synonym:
Target: ERK
27-p-Coumaroyloxyursolic acid
Cat.No: TN2834
Synonym:
Target: Others
10-O-Trans-p-methoxycinnamoylcatalpol
Cat.No: T83467
Synonym:
Target:
Effusanin B
Cat.No: TN3921
Synonym:
Target: Antifection
Talaromycesone A
Cat.No: T38349
Synonym:
Target:
3'-O-Methylorobol
Cat.No: TN1265
Synonym: 3'-O-METHYLOROBOL,3'-O-甲基香豌豆苷元
Target: Others
Izalpinine
Cat.No: TN4342
Synonym:
Target: Others
Anhydroepiophiobolin A
Cat.No: T37543
Synonym:
Target:
Deoxyfusapyrone
Cat.No: T38104
Synonym:
Target:
Coronalolide
Cat.No: TN3704
Synonym:
Target: HIV Protease
Pyranonigrin A
Cat.No: T36513
Synonym:
Target:
3',5,5',7-Tetrahydroxy-4',6-dimethoxyflavone
Cat.No: TN5133
Synonym:
Target: HIV Protease, Topoisomerase
(19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol
Cat.No: T83578
Synonym:
Target:
Effusanin A
Cat.No: TN3920
Synonym:
Target: Raf, Antifection
Mesuol
Cat.No: TN5880
Synonym:
Target:
Herquline A
Cat.No: T38015
Synonym:
Target:
Garcinone E
Cat.No: TN4113
Synonym:
Target: Antifection
19-O-Acetylchaetoglobosin A
Cat.No: T35609
Synonym:
Target:
Mitraciliatine
Cat.No: T83913
Synonym:
Target:
Chevalone C
Cat.No: T36815
Synonym:
Target:
Methyl pyropheophorbide-a
Cat.No: T33492
Synonym: MPPa (Methyl pyropheophorbide-a),NSC267052,Pyropheophorbidea,MPPa,NSC-267052,NSC 267052
Target:
Antibiotic PF 1052
Cat.No: T38097
Synonym:
Target:
11-Oxoisomogroside V
Cat.No: T79965
Synonym:
Target:
Broussonin B
Cat.No: TN5655
Synonym:
Target:
Monocerin
Cat.No: T36992
Synonym:
Target:
Fuscin
Cat.No: T37714
Synonym:
Target:
Sporogen-AO 1
Cat.No: T36438
Synonym:
Target:
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