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1286

抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T33701 NM-3

NM-3,isocoumarin,NM 3,Isocoumarin NM-3,NM3

Apoptosis; Reactive Oxygen Species Apoptosis; Immunology/Inflammation; Metabolism; NF-κB
NM-3 是一种可口服的抗血管生成的抑制剂,具有抗肿瘤活性。NM-3在体外和体内可当作辐射调节剂使用。NM-3抑制血管内皮生长因子(VEGF),从而抑制内皮细胞的增殖。NM-3与活性氧的机制诱导细胞凋亡有关。
TQ0132 A 419259 trihydrochloride

RK 20449 trihydrochloride

Src Angiogenesis; Tyrosine Kinase/Adaptors
A 419259 trihydrochloride (RK 20449 trihydrochloride) 是一种 Src 家族激酶抑制剂,能够抑制 Src (IC50:9 nM)、Lck (IC50:3 nM)、Lyn (IC50:3 nM)。
T10708 CCR1 antagonist 6

CCR Immunology/Inflammation; Microbiology/Virology
CCR1 antagonist 6是一种 CCR1 拮抗剂(IC50 :3 nM)。
T10718L CCT241533 hydrochloride

Chk Cell Cycle/Checkpoint
CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).
T14681 BMS-935177

BTK Angiogenesis; Tyrosine Kinase/Adaptors
BMS-935177 是一种可逆的 BTK 抑制剂,IC50 值为 3 nM
T2272 BPR1J-097

BPR1J097

FLT Angiogenesis; Tyrosine Kinase/Adaptors
BPR1-J097 是新型的、强效的FLT3抑制剂 (IC50:11 nM)。
T2634 Ro3280

RO 3280,Ro5203280

PLK Cell Cycle/Checkpoint
Ro3280 (Ro5203280) 是一种高度选择性的PLK1抑制剂,IC50和Kd 值分别为 3 nM 和 0.09 nM
T10740 CDK8-IN-1

CDK Cell Cycle/Checkpoint
CDK8-IN-1 是一个有效的、CDK8 的选择性抑制剂,其 IC50 值为 3 nM
T6756 AMG 925

FLT; CDK Angiogenesis; Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
AMG 925 是一种选择性FLT3/CDK4双重抑制剂,IC50分别为 1 nM3 nM
TQ0187 SR-3677

ROCK; Autophagy Autophagy; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
SR-3677 是一种有效且特异性的 ROCK2 抑制剂,IC50值为3 nM
T11696 Ivachtin

Caspase-3 Inhibitor VII

Caspase Apoptosis; Proteases/Proteasome
Ivachtin (Caspase-3 Inhibitor VII) 是一种非肽,非竞争性和可逆的caspase-3抑制剂,IC50为 23 nM。它是其余胱天蛋白酶的适度抑制剂。
T6309 AZ960

AZ 960

Apoptosis; Virus Protease; JAK; Parasite Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Microbiology/Virology; Stem Cells
AZ960 是一种高效选择性的 JAK2激酶抑制剂,Ki 值为0.45 nM
T2514 Linifanib

利尼伐尼,ABT-869,RG3635,AL-39324

Apoptosis; c-Fms; VEGFR; FLT; CSF-1R; PDGFR; c-Kit; Autophagy Angiogenesis; Apoptosis; Autophagy; Tyrosine Kinase/Adaptors
Linifanib (AL-39324) 是一种高效口服的VEGFR 和PDGFR 家族多靶点抑制剂,具有显著的抗肿瘤活性。它对无关 RTKs、可溶性酪氨酸激酶或丝氨酸/苏氨酸激酶的活性要低得多。它是特异性 miR-10b 抑制剂,阻断miR-10b 的生物合成。
T10244 ACY-1083

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
ACY-1083 是一种选择性和脑穿透性 HDAC6 抑制剂 (IC50:3 nM),可有效逆转化疗引起的周围神经病变。
T2251 NVP-TAE 684

TAE684,5-氯-N2-[2-甲氧基-4-[4-(4-甲基-1-哌嗪基)-1-哌啶基]苯基]-N4-[2-[(1-甲基乙基)磺酰基]苯基]-2,4-嘧啶二胺

Apoptosis; ALK Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
NVP-TAE 684 (TAE684) 是一种高效特异性 ALK 抑制剂,阻止 ALCL 衍生的 ALK 依赖性细胞株的生长,IC50值为 3 nM
T7202 ITE

AhR; Aryl Hydrocarbon Receptor Immunology/Inflammation; Metabolism
ITE 是一种有效的芳烃受体 (AhR) 内源性激动剂,Ki 值为 3 nM。它具有免疫抑制作用。
T8751 AZD8931 diFuMaric acid

4-[[4-[(3-氯-2-氟苯基)氨基]-7-甲氧基-6-喹唑啉基]氧基]-N-甲基-1-哌啶乙酰胺二富马酸盐

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
AZD8931 diFuMaric acid 是一种可逆的 ATP 竞争性 EGFR、ErbB2 和 ErbB3 抑制剂(IC50 分别为 4 nM3 nM 和 4 nM)。
TQ0014 GNE-131

Sodium Channel Membrane transporter/Ion channel
GNE-131 是有效的人类钠离子通道 NaV1.7(hNaV1.7)选择性抑制剂,IC50为 3 nM
T2650 MK-8245

Dehydrogenase; Stearoyl-CoA Desaturase (SCD) Metabolism
MK8245 是肝靶向的硬脂酰 -CoA 去饱和酶(SCD)抑制剂,对人 SCD1 和鼠 SCD1 的IC50值分别为 1 nM3 nM,具有抗糖尿病和抗血脂异常的作用。
TP1380 Galanin (1-16), mouse, porcine, rat

Neuropeptide Y Receptor GPCR/G Protein; Neuroscience
Galanin (1-16), mouse, porcine, rat 是一种有效的甘丙肽受体激动剂,Kd 为 3 nM
T2710 TCS 1102

OX Receptor GPCR/G Protein; Neuroscience
TCS 1102 是双食欲素受体拮抗剂,对 OX1和OX2受体的Ki 分别为3和 0.2 nM
T4295 (R)-GNE-140

GNE-140

Dehydrogenase Metabolism
(R)-GNE-140 (GNE-140) 是 LDHA 抑制剂,能够作用于 LDHA (IC50:3 nM) 和 LDHB (IC50:3 nM)。它的活性是 S 型异构体的 18 倍。
T3599 BFH772

BFH-722

VEGFR Angiogenesis; Tyrosine Kinase/Adaptors
BFH772 是 VEGFR2抑制剂(IC50:3 nM),具有口服活性。
T40465 SAG dihydrochloride

Hedgehog/Smoothened GPCR/G Protein; Stem Cells
SAG dihydrochloride 是一种强效的 Smoothened(Smo)受体激动剂(EC 50 =3 nM;K d =59 nM)。SAG dihydrochloride 可激活刺猬信号通路并抵消环丙胺对 Smo 的抑制。
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。
TQ0263 EPZ031686

EPZ-031686

Histone Methyltransferase Chromatin/Epigenetic
EPZ031686 是一种有效的 SMYD3 抑制剂,IC50 为 3 nM,可用于癌症研究。
T2630 Poziotinib

HM781-36B,NOV120101

Apoptosis; EGFR; HER Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Poziotinib (NOV120101) 是一种不可逆的 HER1/2/4 抑制剂 (IC50s: 3/5/23 nM)。
T1994 Pictilisib

RG7321,GDC-0941

Apoptosis; PI3K; Autophagy Apoptosis; Autophagy; PI3K/Akt/mTOR signaling
Pictilisib (GDC-0941) 是一种PI3Kα/δ抑制剂,IC50为 3 nM。它对110β和 p110γ 具有适度的选择性,分别为11倍和25倍。
T7083 GLPG1837

ABBV-974

CFTR; Autophagy Autophagy; Membrane transporter/Ion channel
GLPG1837 (ABBV-974) 是一种有效的 CFTR 增强剂,对其 F508del 和 G551D 的 EC50 分别为 3 nM339 nM
TQ0035 Fulacimstat

BAY1142524

Others Others
Fulacimstat (BAY1142524) 是可口服的糜酶抑制剂,能够作用于人糜酶(IC50:4 nM)和仓鼠糜酶(IC50:3 nM)。
T2638 Gandotinib

LY2784544

VEGFR; FGFR; FLT; JAK Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
Gandotinib (LY2784544) 是一种JAK2抑制剂,IC50为 3 nM。它也抑制FLT3、FLT4、FGFR2、TYK2 和 TRKB,IC50分别为 4、25、32、44 和 95 nM
T14561 BI-3812

BCL Apoptosis
BI-3812 是一种高效的BCL6抑制剂,具有抗肿瘤活性,能够抑制 BCL6 的 BTB 结构域,IC50值 ≤3 nM
T17263 XEN907

Others Others
XEN907 is a novel spiro oxindole NaV1.7 blocker. XEN907 also inhibits hNaV1.7 (IC50: 3 nM).
TQ0097 AGN 193109

Retinoid Receptor; Autophagy Autophagy; Metabolism
AGN 193109 是一种类视黄醇类似物,是一种有效的特异性 RAR 拮抗剂,可抑制 RARα、RARβ和 RARγ的活性,Kd 值分别为 2 nM、2 nM3 nM
T6638 Retapamulin

瑞他莫林,SB-275833

ribosome; Antibacterial; Antibiotic Microbiology/Virology
Retapamulin (SB-275833) 是一种能结合金黄色葡萄球菌和大肠杆菌核糖体的局部抗生素,Kd 为3 nM
T12906 SI-2 hydrochloride

EPH 116 hydrochloride

Src Angiogenesis; Tyrosine Kinase/Adaptors
SI-2 hydrochloride (EPH 116 hydrochloride) 是 SRC-3 的抑制剂,诱导乳腺癌细胞死亡的 IC50 值为 3-20 nM。SI-2 hydrochloride 具有良好的药代动力学特征和改善的毒性,以及可接受的口服可用性。
T16021 MBQ-167

CDK; Ras Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
MBQ-167 是一种 Rac/Cdc42 的双重抑制剂,在 MDA-MB-231 细胞中,Rac 1/2/3 和 Cdc42 的 IC50 分别为 103 nM 和 78 nM
T6143 PI-103

PI103,PI 103

Apoptosis; DNA-PK; PI3K; mTOR; Autophagy Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
PI-103 是一种 PI3K 和 mTOR 抑制剂,抑制 p110α、p110β、p110δ、p110γ、mTORC1和 mTORC2,IC50分别为 8 nM、88 nM、48 nM、150 nM、20 nM 和 83 nM。它可诱导自噬,还抑制 DNA-PK,IC50为 2 nM
T6283 Wortmannin

SL-2052,渥曼青霉素,KY-12420

ATM/ATR; DNA-PK; Serine/threonin kinase; PLK; PI3K; Antibiotic; Autophagy Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling
Wortmannin (SL-2052) 是一种 PI3K 抑制剂 (IC50=3 nM),具有共价性和不可逆性。Wortmannin 也是一种 PlK1 和 PlK3 的抑制剂 (IC50=5.8/48 nM),可以阻断自噬。
T6092 Sapitinib

沙普替尼,AZD-8931

EGFR Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Sapitinib (AZD-8931) 是可逆的 ATP 竞争型 EGFR 抑制剂,对 EGFR、ErbB2 和 ErbB3的IC50值分别为4、3 和 4 nM
T11381 Pictilisib dimethanesulfonate

GDC-0941 dimethanesulfonate,GDC-0941 2 MeSO3H salt

Apoptosis; DNA-PK; PI3K; mTOR; Autophagy Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) 是一种 PI3Kα/δ抑制剂,IC50值为 3 nM。对 p110β 和 p110γ的选择性分别为11倍和25倍。
T6312 R547

Ro 4584820

Apoptosis; GSK-3; PKA; CDK Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
R547 (Ro 4584820) 是一种口服有效,选择性, ATP 竞争性CDK 抑制剂,对 CDK1/cyclin B、 CDK2/cyclin E 和 CDK4/cyclin D1 作用的Ki 值分别为 2 nM3 nM、1 nM
T12539L Prinomastat

KB-R9896,普啉司他,AG3340

MMP Proteases/Proteasome
Prinomastat inhibits MMP-2, MMP-3 and MMP-9 (Kis: 0.05 nM, 0.3 nM and 0.26 nM, respectively). Prinomastat crosses the blood-brain barrier. It also has antitumor activity. Prinomastat is a broad-spectrum, potent, orally active metalloproteinase inhibitor (
T5099 Gefapixant

RO 4926219,AF219,MK-7264

P2X Receptor Membrane transporter/Ion channel; Neuroscience
Gefapixant (AF219) 是一个 P2X3 受体拮抗剂,其对人同源重组 hP2X3 和 hP2X2/3 的 IC50值分别是约 30 和 100-250 nM
T13423L (1S,2R)-2-PCCA

(1S,2R)-2-PCCA(Iso-1609563-71-4)

GPR Endocrinology/Hormones; GPCR/G Protein
(1S,2R)-2-PCCA 是一种新型有效的小分子 GPR88 受体激动剂,非细胞体系下测的 EC50 值为 3 nM,细胞体系下测得 EC50 值为 603 nM
T6296 RAF265

CHIR-265

Apoptosis; Raf; VEGFR; Autophagy Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors
RAF265 (CHIR-265) 是一种 RAF/VEGFR2抑制剂。
T1779 SAG

Smoothened Agonist (SAG) HCl,Smoothened Agonist

Hedgehog/Smoothened; Smo GPCR/G Protein; Stem Cells
SAG (Smoothened Agonist) 是一种 Smo 受体激动剂 (EC50=3 nM),具有细胞渗透性和选择性。SAG 可以直接结合 Smo 螺旋束调节 Smo 活性,可以活化 Hedgehog 信号通路。
T12835 Saroglitazar

Lipaglyn

PPAR DNA Damage/DNA Repair; Metabolism
Saroglitazar (Lipaglyn) 是 PPAR 的激动剂,对 PPARα 和 PPARγ 的 EC50 值为 0.65 pM 和 3 nM
T1957 AZD2858

GSK-3 PI3K/Akt/mTOR signaling; Stem Cells
AZD2858 是具有口服活性的GSK-3抑制剂,可以抑制 GSK-3α (IC50:0.9 nM) 和 GSK-3β (IC50:5 nM) 的活性,可用于骨折愈合的研究。
T3700 SCH900776 (S-isomer)

MK-8776 S-isomer,SCH900776 S-isomer

Chk; CDK Cell Cycle/Checkpoint
SCH900776 S-isomer (MK-8776 S-isomer) 是SCH900776的S 型同分异构体。

化合物

NM-3
Cat.No: T33701
Synonym: NM-3,isocoumarin,NM 3,Isocoumarin NM-3,NM3
Target: Apoptosis, Reactive Oxygen Species
A 419259 trihydrochloride
Cat.No: TQ0132
Synonym: RK 20449 trihydrochloride
Target: Src
CCR1 antagonist 6
Cat.No: T10708
Synonym:
Target: CCR
CCT241533 hydrochloride
Cat.No: T10718L
Synonym:
Target: Chk
BMS-935177
Cat.No: T14681
Synonym:
Target: BTK
BPR1J-097
Cat.No: T2272
Synonym: BPR1J097
Target: FLT
Ro3280
Cat.No: T2634
Synonym: RO 3280,Ro5203280
Target: PLK
CDK8-IN-1
Cat.No: T10740
Synonym:
Target: CDK
AMG 925
Cat.No: T6756
Synonym:
Target: FLT, CDK
SR-3677
Cat.No: TQ0187
Synonym:
Target: ROCK, Autophagy
Ivachtin
Cat.No: T11696
Synonym: Caspase-3 Inhibitor VII
Target: Caspase
AZ960
Cat.No: T6309
Synonym: AZ 960
Target: Apoptosis, Virus Protease, JAK, Parasite
Linifanib
Cat.No: T2514
Synonym: 利尼伐尼,ABT-869,RG3635,AL-39324
Target: Apoptosis, c-Fms, VEGFR, FLT, CSF-1R, PDGFR, c-Kit, Autophagy
ACY-1083
Cat.No: T10244
Synonym:
Target: HDAC
NVP-TAE 684
Cat.No: T2251
Synonym: TAE684,5-氯-N2-[2-甲氧基-4-[4-(4-甲基-1-哌嗪基)-1-哌啶基]苯基]-N4-[2-[(1-甲基乙基)磺酰基]苯基]-2,4-嘧啶二胺
Target: Apoptosis, ALK
ITE
Cat.No: T7202
Synonym:
Target: AhR, Aryl Hydrocarbon Receptor
AZD8931 diFuMaric acid
Cat.No: T8751
Synonym: 4-[[4-[(3-氯-2-氟苯基)氨基]-7-甲氧基-6-喹唑啉基]氧基]-N-甲基-1-哌啶乙酰胺二富马酸盐
Target: EGFR
GNE-131
Cat.No: TQ0014
Synonym:
Target: Sodium Channel
MK-8245
Cat.No: T2650
Synonym:
Target: Dehydrogenase, Stearoyl-CoA Desaturase (SCD)
Galanin (1-16), mouse, porcine, rat
Cat.No: TP1380
Synonym:
Target: Neuropeptide Y Receptor
TCS 1102
Cat.No: T2710
Synonym:
Target: OX Receptor
(R)-GNE-140
Cat.No: T4295
Synonym: GNE-140
Target: Dehydrogenase
BFH772
Cat.No: T3599
Synonym: BFH-722
Target: VEGFR
SAG dihydrochloride
Cat.No: T40465
Synonym:
Target: Hedgehog/Smoothened
Src Inhibitor 3
Cat.No: T13000
Synonym:
Target: Others, Src
EPZ031686
Cat.No: TQ0263
Synonym: EPZ-031686
Target: Histone Methyltransferase
Poziotinib
Cat.No: T2630
Synonym: HM781-36B,NOV120101
Target: Apoptosis, EGFR, HER
Pictilisib
Cat.No: T1994
Synonym: RG7321,GDC-0941
Target: Apoptosis, PI3K, Autophagy
GLPG1837
Cat.No: T7083
Synonym: ABBV-974
Target: CFTR, Autophagy
Fulacimstat
Cat.No: TQ0035
Synonym: BAY1142524
Target: Others
Gandotinib
Cat.No: T2638
Synonym: LY2784544
Target: VEGFR, FGFR, FLT, JAK
BI-3812
Cat.No: T14561
Synonym:
Target: BCL
XEN907
Cat.No: T17263
Synonym:
Target: Others
AGN 193109
Cat.No: TQ0097
Synonym:
Target: Retinoid Receptor, Autophagy
Retapamulin
Cat.No: T6638
Synonym: 瑞他莫林,SB-275833
Target: ribosome, Antibacterial, Antibiotic
SI-2 hydrochloride
Cat.No: T12906
Synonym: EPH 116 hydrochloride
Target: Src
MBQ-167
Cat.No: T16021
Synonym:
Target: CDK, Ras
PI-103
Cat.No: T6143
Synonym: PI103,PI 103
Target: Apoptosis, DNA-PK, PI3K, mTOR, Autophagy
Wortmannin
Cat.No: T6283
Synonym: SL-2052,渥曼青霉素,KY-12420
Target: ATM/ATR, DNA-PK, Serine/threonin kinase, PLK, PI3K, Antibiotic, Autophagy
Sapitinib
Cat.No: T6092
Synonym: 沙普替尼,AZD-8931
Target: EGFR
Pictilisib dimethanesulfonate
Cat.No: T11381
Synonym: GDC-0941 dimethanesulfonate,GDC-0941 2 MeSO3H salt
Target: Apoptosis, DNA-PK, PI3K, mTOR, Autophagy
R547
Cat.No: T6312
Synonym: Ro 4584820
Target: Apoptosis, GSK-3, PKA, CDK
Prinomastat
Cat.No: T12539L
Synonym: KB-R9896,普啉司他,AG3340
Target: MMP
Gefapixant
Cat.No: T5099
Synonym: RO 4926219,AF219,MK-7264
Target: P2X Receptor
(1S,2R)-2-PCCA
Cat.No: T13423L
Synonym: (1S,2R)-2-PCCA(Iso-1609563-71-4)
Target: GPR
RAF265
Cat.No: T6296
Synonym: CHIR-265
Target: Apoptosis, Raf, VEGFR, Autophagy
SAG
Cat.No: T1779
Synonym: Smoothened Agonist (SAG) HCl,Smoothened Agonist
Target: Hedgehog/Smoothened, Smo
Saroglitazar
Cat.No: T12835
Synonym: Lipaglyn
Target: PPAR
AZD2858
Cat.No: T1957
Synonym:
Target: GSK-3
SCH900776 (S-isomer)
Cat.No: T3700
Synonym: MK-8776 S-isomer,SCH900776 S-isomer
Target: Chk, CDK
Cat. No. Product Name Target Signaling Pathways
T0320 Colchicine

秋水仙碱,秋水仙素,Colcin,Colchineos,Colchisol

Apoptosis; Microtubule Associated; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling
Colchicine (Colcin) 属于天然产物,是一种微管聚合的抑制剂 (IC50=3 nM),通过与微管蛋白结合来阻断微管的聚合。Colchicine 可以被用于治疗通风和风湿病。
TN1254 3'-Methoxydaidzein

3'-甲氧基大豆苷元

Sodium Channel Membrane transporter/Ion channel
3'-Methoxydaidzein 是一种异黄酮和 Sodium Channel 双重抑制剂。3'-Methoxydaidzein 对NaV1.7、NaV1.8 和 NaV1.3有抑制作用,IC50 分别为 181 nM397 nM 和 505 nM3'-Methoxydaidzein 对胶原诱导的血小板聚集具有特异性,IC50值分别为12.3和61.5µM。。3'-Methoxydaidzein 通过抑制电压门控钠通道发挥镇痛作用。 3'-Methoxydaidzein 具有抗氧化活性和抗血小板聚集活性。
T15686 L-741626

3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole

Dopamine Receptor GPCR/G Protein; Neuroscience
L-741626 (3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole) 是D2多巴胺受体选择性拮抗剂,对人 D2、D3 和 D4 受体的Ki 分别为 2.4、100 和 220 nM
TN1328 7-Amino-4-methylcoumarin-3-acetic acid

7-氨基-4-甲基-3-香豆素醋酸,7-Amino-4-methylcoumarin

Others Others
7-Amino-4-methylcoumarin-3-acetic acid (7-Amino-4-methylcoumarin) 是荧光蛋白质标记剂,能够被紫外光(350 nm) 激活,可在蓝色区域 (440-460 nm) 发光。
TN1047 Ingenol mebutate

Ingenol 3-Angelate,巨大戟醇甲基丁烯酸酯,PEP005

gp120/CD4; HIV Protease; PKC Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
Ingenol mebutate (Ingenol 3-Angelate) 是 PKC 的有效激动剂,包括 PKC-α、PKC-β、PKC-γ、PKC-δ 和 PKC-ε,Kis 为 0.3、0.105、0.162、0.376 和 0.171 nM。 Ingenol mebutate 具有抗炎和抗肿瘤活性。
T6680 Staurosporine

Antibiotic AM-2282,星形孢菌素,AM-2282,CGP 41251,星孢菌素

Apoptosis; PKA; Antibacterial; Antibiotic; Src; PKC; Antifungal Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors
Staurosporine (AM-2282) 是一种蛋白激酶抑制剂,对 PKC、PKA、c-Fgr、Phosphorylase kinase 和 TAOK2 均有抑制活性 (IC50=6/15/2/3/3000 nM),具有 ATP 竞争性和非选择性。Staurosporine 也可以诱导凋亡。
T21855 AMI-193

Espiramida,螺拉米特,Spiramide

Dopamine Receptor; 5-HT Receptor GPCR/G Protein; Neuroscience
AMI-193 (Spiramide) 是一种有效和选择性的 5-HT2 和 D2 受体,对 5-HT2、D2 受体、5-HT1A、D1 受体和 5-HT1C 受体的 Kis 分别为 2、3、50、2530 和 4300 nM。 AMI-193 显示出抗精神病活性。
TN2256 Taccalonolide B

根薯酮内酯B,根薯酮内酯 B

Microtubule Associated Cytoskeletal Signaling
Taccalonolide B 是从广西裂果薯中分离得到的一种微管稳定剂,具有抗肿瘤活性。它抑制 SK-OV-3 细胞的生长,IC50 为 208 nM,在体外对过表达 P-糖蛋白 (Pgp) 和多药耐药蛋白 (MRP7) 的细胞系有效。
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
T2S1635 3-Isomangostin

MTH1 DNA Damage/DNA Repair
3-Isomangostin 可从莽吉柿壳中提取的一种天然产物,是一种乙酰胆碱酯酶选择性抑制剂,也是一种有效的人醛糖还原酶抑制剂,IC50 为 3.48 uM。它抑制 MutT 同源物 1 (MTH1),IC50 为 52 nM。它具有清除自由基、抗疟原虫和抗癌的活性。
T4429 Rauwolscine hydrochloride

Corynanthidine hydrochloride,盐酸育亨宾碱,萝芙素盐酸盐,α-Yohimbine hydrochloride,Isoyohimbine hydrochloride

Adrenergic Receptor GPCR/G Protein; Neuroscience
Rauwolscine hydrochloride (Isoyohimbine hydrochloride) 是一种高选择性的 α2 adrenergic 受体拮抗剂,Ki=12 nM
T5S0890 Oleandrin

Neriostene,Folinerin,Foliandrin,欧夹竹桃苷

Apoptosis; ATPase; Potassium Channel; Sodium Channel Apoptosis; Membrane transporter/Ion channel
Oleandrin (Folinerin) 是夹竹桃属中的一种类固醇,可抑制Na+/K+-ATPase 活性,IC50为 620 nM
T3857 magnolin

木兰脂素,(+)-Magnolin,木兰苷

ERK MAPK
Magnolin 是辛夷的一种主要成分,靶向作用于ERK1和ERK2,IC50值分别为 87 和 16.5 nM,可抑制Ras/ERKs/RSK2信号通路。它在体内外降低肾脏氧化应激,抑制 caspase-3 活性,并增加 Bcl-2 表达,具有抗炎和抗氧化作用。
TL0007 Bisdemethoxycurcumin

双去甲氧基姜黄素,Curcumin III,Didemethoxycurcumin

Epigenetic Reader Domain; Wnt/beta-catenin Chromatin/Epigenetic; Cytoskeletal Signaling; Stem Cells
Bisdemethoxycurcumin (Curcumin III) 是一种具有抗炎及抗氧化作用的姜黄素。
T3377 L-Phenylalanine

L-苯丙氨酸,(S)-2-Amino-3-phenylpropionic acid,phenylalanine,3-Phenyl-L-alanine

Calcium Channel; Endogenous Metabolite; iGluR Membrane transporter/Ion channel; Metabolism; Neuroscience
L-Phenylalanine (3-Phenyl-L-alanine) 是分离自大肠杆菌的必需氨基酸,是 NMDARs(KB573 μM) 和非 NMDARs 的甘氨酸和谷氨酸结合位点的竞争性拮抗剂,用于食品香料和药品的生产中。它是一种电压依赖性 α2δ 亚基 Ca2+通道拮抗剂,Ki 为 980 nM
TN2254 Taccalonolide A

根薯酮内酯A,根薯酮内酯 A

Apoptosis; Microtubule Associated Apoptosis; Cytoskeletal Signaling
Taccalonolide A 是从水田七根茎中分离得到的一种类固醇,具有细胞毒性和抗疟活性。它在体外对过表达 p 糖蛋白、多药耐药蛋白 7 细胞系有抑制作用,抑制 SK-OV-3 细胞生长的 IC50值为 622 nM。它是微管稳定剂,能引起 G2-M 期滞留、Bcl-2 磷酸化,并引发细胞凋亡。
T6S0232 Eriodictyol

圣草酚,Huazhongilexone

Influenza Virus; DNA/RNA Synthesis; Nrf2; Endogenous Metabolite Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology
Eriodictyol (Huazhongilexone) 是从中草药中得到的一种黄酮类天然产物,具有抗氧化、抗炎和抗糖尿病作用。它还是一种流感依赖 RNA 的RNA 聚合酶抑制剂,IC50为 18 nM。它可诱导Nrf2信号通路。
T6S2391 L-Chicoric Acid

(-)-Chicoric acid,trans-Caffeoyltartaric acid,Chicoric acid,L-菊苣酸,dicaffeoyltartaric acid,菊苣酸

Others; HIV Protease Microbiology/Virology; Others; Proteases/Proteasome
L-Chicoric Acid (trans-Caffeoyltartaric acid) 是一种二咖啡酰酒石酸,是一种选择性可逆的 HIV-1 整合酶抑制剂,IC50约为 100 nM。它还可抑制 HIV-1 复制。
T6S1487 Ginsenoside Rg5

人参皂苷Rg5,人参皂甙 Rg5

NF-κB; COX; IGF-1R Immunology/Inflammation; Neuroscience; NF-κB; Tyrosine Kinase/Adaptors
Ginsenoside Rg5 是红参的主要成分,可阻断IGF-1与其受体的结合,IC50约为90 nM。它还通过抑制NF-κB p65的 DNA 结合活性来抑制COX-2的 mRNA 表达。它可促进血管生成和改善高血压,具有抗炎和治疗阿尔茨海默病的潜力。
T39367 Suomilide

Suomilide effectively inhibits human trypsin-2 and trypsin-3, displaying IC50 values of 4.7 nM and 11.5 nM, respectively. Additionally, it exhibits inhibition of trypsin-1 with an IC50 value of 104 nM.
T14121 Actinonin

(-)-Actinonin

Aminopeptidase Metabolism
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM, it also is an apoptosis inducer. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase, it also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].
T15542 Hypothemycin

Others Others
Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively).
TN6062 1,3,9-Trimethyluric acid

1,3,9-Trimethyluric acid exhibits in vitro cytotoxic activity against breast cancer (MCF-7), human neuroblastoma (SHSY5Y), human non-small cell lung cancer (A549) and human liver cancer (HEPG2) with IC50 value in the range of 1-3 uM. 1,3,9-Trimethyluric a
T36749 Herboxidiene

Herboxidiene is a polyketide originally isolated from S. chromofuscus that has diverse biological activities.[1],[2,][3],[4],[5] It inhibits growth of HeLa S3, SK-MEL-2, PC3, A549, and EBC-1 cells with GI50 values ranging from 7.4 to 62 nM.3 Herboxidiene is cytostatic against human umbilical vein endothelial cells (HUVECs; (IC50 = 26 nM)) and inhibits VEGF-induced invasion and tube formation of serum-starved HUVECs in a concentration-dependent manner, indicating antiangiogenic activity.[4] Herbo...
T37609 (rel)-Asperparaline A

Aspergillimide is a fungal metabolite originally isolated from A. japonicus.1 It reduces nicotinic acetylcholine receptor (nAChR) peak and slowly-desensitizing amplitudes induced by acetylcholine in silkworm (B. mori) larval neurons (IC50s = 20.2 and 39.6 nM, respectively) but has no effect on chicken α3β4-, α4β2-, and α7-containing nAChRs.2 Dietary administration of aspergillimide A (10 μg/g of diet) induces paralysis in silkworm fourth instar larvae.1 Aspergillimide A (10 and 20 mg/kg) reduces...
T75436 Jatrorrhizine hydroxide

Jatrorrhizine hydroxide, 一种从黄连中提取的生物碱,展现了神经保护、抗菌、抗疟原虫及抗氧化的活性。作为一种高效的乙酰胆碱酯酶(AChE)抑制剂(IC50=872 nM),其对BuChE的选择性高达115倍。此外,Jatrorrhizine hydroxide还能通过抑制uptake-2 transporter活性来减少血清素(5-HT)和去甲肾上腺素(NE)的摄取,表现出口服活性。

天然产物

Colchicine
Cat.No: T0320
Synonym: 秋水仙碱,秋水仙素,Colcin,Colchineos,Colchisol
Target: Apoptosis, Microtubule Associated, Autophagy
3'-Methoxydaidzein
Cat.No: TN1254
Synonym: 3'-甲氧基大豆苷元
Target: Sodium Channel
L-741626
Cat.No: T15686
Synonym: 3-(4-(4-Chlorophenyl-4-hydroxypiperidino)methyl)indole
Target: Dopamine Receptor
7-Amino-4-methylcoumarin-3-acetic acid
Cat.No: TN1328
Synonym: 7-氨基-4-甲基-3-香豆素醋酸,7-Amino-4-methylcoumarin
Target: Others
Ingenol mebutate
Cat.No: TN1047
Synonym: Ingenol 3-Angelate,巨大戟醇甲基丁烯酸酯,PEP005
Target: gp120/CD4, HIV Protease, PKC
Staurosporine
Cat.No: T6680
Synonym: Antibiotic AM-2282,星形孢菌素,AM-2282,CGP 41251,星孢菌素
Target: Apoptosis, PKA, Antibacterial, Antibiotic, Src, PKC, Antifungal
AMI-193
Cat.No: T21855
Synonym: Espiramida,螺拉米特,Spiramide
Target: Dopamine Receptor, 5-HT Receptor
Taccalonolide B
Cat.No: TN2256
Synonym: 根薯酮内酯B,根薯酮内酯 B
Target: Microtubule Associated
Methyl pyropheophorbide-a
Cat.No: T33492
Synonym: MPPa (Methyl pyropheophorbide-a),NSC267052,Pyropheophorbidea,MPPa,NSC-267052,NSC 267052
Target:
3-Isomangostin
Cat.No: T2S1635
Synonym:
Target: MTH1
Rauwolscine hydrochloride
Cat.No: T4429
Synonym: Corynanthidine hydrochloride,盐酸育亨宾碱,萝芙素盐酸盐,α-Yohimbine hydrochloride,Isoyohimbine hydrochloride
Target: Adrenergic Receptor
Oleandrin
Cat.No: T5S0890
Synonym: Neriostene,Folinerin,Foliandrin,欧夹竹桃苷
Target: Apoptosis, ATPase, Potassium Channel, Sodium Channel
magnolin
Cat.No: T3857
Synonym: 木兰脂素,(+)-Magnolin,木兰苷
Target: ERK
Bisdemethoxycurcumin
Cat.No: TL0007
Synonym: 双去甲氧基姜黄素,Curcumin III,Didemethoxycurcumin
Target: Epigenetic Reader Domain, Wnt/beta-catenin
L-Phenylalanine
Cat.No: T3377
Synonym: L-苯丙氨酸,(S)-2-Amino-3-phenylpropionic acid,phenylalanine,3-Phenyl-L-alanine
Target: Calcium Channel, Endogenous Metabolite, iGluR
Taccalonolide A
Cat.No: TN2254
Synonym: 根薯酮内酯A,根薯酮内酯 A
Target: Apoptosis, Microtubule Associated
Eriodictyol
Cat.No: T6S0232
Synonym: 圣草酚,Huazhongilexone
Target: Influenza Virus, DNA/RNA Synthesis, Nrf2, Endogenous Metabolite
L-Chicoric Acid
Cat.No: T6S2391
Synonym: (-)-Chicoric acid,trans-Caffeoyltartaric acid,Chicoric acid,L-菊苣酸,dicaffeoyltartaric acid,菊苣酸
Target: Others, HIV Protease
Ginsenoside Rg5
Cat.No: T6S1487
Synonym: 人参皂苷Rg5,人参皂甙 Rg5
Target: NF-κB, COX, IGF-1R
Suomilide
Cat.No: T39367
Synonym:
Target:
Actinonin
Cat.No: T14121
Synonym: (-)-Actinonin
Target: Aminopeptidase
Hypothemycin
Cat.No: T15542
Synonym:
Target: Others
1,3,9-Trimethyluric acid
Cat.No: TN6062
Synonym:
Target:
Herboxidiene
Cat.No: T36749
Synonym:
Target:
(rel)-Asperparaline A
Cat.No: T37609
Synonym:
Target:
Jatrorrhizine hydroxide
Cat.No: T75436
Synonym:
Target:
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