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296

抑制剂 & 化合物

32

天然产物

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Cat. No. Product Name Target Signaling Pathways
T12030 MG 1

Adrenergic Receptor GPCR/G Protein; Neuroscience
MG 1是一种有效的 α1肾上腺素能受体拮抗剂。
T6583 MG-101

ALLN,Ac-LLnL-CHO,Calpain inhibitor I,Calpain inhibitor-1,MG101,钙蛋白酶抑制剂I

Cysteine Protease; Proteasome Proteases/Proteasome; Ubiquitination
MG-101 (Calpain inhibitor I) 是一种有效的半胱氨酸蛋白酶抑制剂,能够抑制钙蛋白酶I (Ki:190 pM),钙蛋白酶II (Ki:220 pM),组织蛋白酶B (Ki:150 pM)和组织蛋白酶L (Ki:500 pM)。
T12628 (R)-MG-132

(S,R,S)-(-)-MG-132,N-[(苯基甲氧基)羰基]-L-亮氨酰-N-[(1S)-1-甲酰基-3-甲基丁基]-D-亮氨酰胺,Z-Leu-D-leu-leu-al

Proteasome Proteases/Proteasome; Ubiquitination
(R)-MG-132 (Z-Leu-D-leu-leu-al) 是一种 MG-132 的对映异构体,是一种蛋白酶体 (proteasome) 抑制剂,细胞毒性比 MG-132 弱,是一种比 MG-132 更有效的proteasome 抑制剂。
T4349 Sitravatinib

MG516,MGCD516

Discoidin Domain Receptor (DDR); VEGFR; FLT; Trk receptor; TAM Receptor; c-Kit; Ephrin Receptor Angiogenesis; Tyrosine Kinase/Adaptors
Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它单独使用即具有有效的抗肿瘤功效,且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。
T18391 N-Boc-4-pentyne-1-amine

Others; PROTAC Linker Others; PROTAC
N-Boc-4-pentyne-1-amine 是一种基于烷基链的PROTAC连结剂,用于PROTAC MG-277[1]的合成。
T35033L (S)-Vamicamide

(S)-Vamicamide (Iso-132373-81-0)

AChE Neuroscience
(S)-Vamicamide 是一种新型抗抗胆碱能化合物。Vamicamide 在 32 mg/kg 或更高 (p.o.) 时增加小鼠的自发运动活动,并在 100 mg/kg 时抑制小鼠强直性惊厥。
T21617 MG-115

Z-LL-Nva-CHO

Proteasome Proteases/Proteasome; Ubiquitination
MG-115 (Z-LL-Nva-CHO) 是一种有效且可逆的蛋白酶体抑制剂,对20S 和26S 蛋白酶体的 Ki 值分别为 21 nM 和 35 nM。MG-115 特异性抑制蛋白酶体的胰凝乳蛋白酶样活性,诱导 p53 依赖性细胞凋亡。
T15237 Eperezolid

PNU-100592

Antibacterial; Antibiotic Microbiology/Virology
Eperezolid (PNU-100592) 是一种在体外表现出良好抑制活性的恶唑烷酮类抗生素。
T1569 Tigecycline

替加环素,GAR-936

ribosome; Antibacterial; Antibiotic; Autophagy Autophagy; Microbiology/Virology
Tigecycline (GAR-936) 是甘氨酰环素抗生素,对 Acinetobacter baumannii(A. baumannii) 的 MIC50和 MIC90分别为 1 和 2 mg/L。它对 E. coli(MG1655 菌株) 的平均抑制浓度 (MIC) 约 125 ng/ mL。
T4039 BIBB 515

Others Others
BIBB 515 是口服具有活力的 2,3-氧化角鲨烯环化酶选择性抑制剂,在大鼠和小鼠中的 ED50值分别为 0.2-0.5 mg/kg 和 0.36-33.3 mg/kg (1-5 小时)。它主要利用抑制低密度脂蛋白的产生,从而发挥降脂作用。
T36569 KR-32568

Sodium Channel Membrane transporter/Ion channel
KR-32568是一种钠/氢交换器1(NHE-1)抑制剂(IC50:230 nM)。KR-32568具有强大的心脏保护作用。当使用浓度为10μM 时,它能在离体的缺血大鼠心脏模型中恢复心脏收缩功能。KR-32568(0.3mg/kg)在缺血和再灌注损伤的大鼠模型中减少了心肌梗死的大小。
T67956 Litoxetine

5-HT Receptor GPCR/G Protein; Neuroscience
Litoxetine 是一种选择性的5-HT 摄取抑制剂,是具有5-HT3受体拮抗剂。Litoxetine 可作为一种抗抑郁剂,在雪貂身上显示出止吐特性。Litoxetine (110毫克/公斤静脉注射)剂量依赖性地减少了反胃和呕吐的次数,延迟了呕吐的发生。Litoxetine 对大脑5HT3受体有亲和力(Ki = 85 nM)。
T22697 CS 2100

1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid

S1P Receptor GPCR/G Protein
CS 2100 (1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid) 是口服有活性 S1P3-sparingS1P1选择性激动剂,对人 S1P1的EC50值为 4.0 nM,对 HvGR 的ID50值为 0.407 mg/kg。它在大鼠体内具有免疫抑制作用。
T4436 RO1138452

CAY10441

Others; Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation; Others
RO1138452 (CAY10441) 是一种选择性和可口服的前列环素受体拮抗剂,pKi 为8.3。它拮抗卡前列环素诱导的人神经母细胞瘤腺苷酸环化酶的激活,以剂量依赖性方式阻断环 AMP 积累,具有镇痛活性。
T4306 CCG-203971

CCG203971

Rho; Ras Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
CCG-203971 是一种Rho/MRTF/SRF 通路抑制剂,具有潜在的抗转移作用。它有效靶向 RhoA/C 激活的 SRE 荧光素酶,IC50为 6.4 μM。它抑制 PC-3 细胞迁移,IC50为 4.2 μM。
T38192 Unifiram

Others Others
Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。
T35689 MTP 131 acetate

Others Others
MTP 131 acetate 是一种小的线粒体靶向四肽。
T38050 CP-609754

Transferase Metabolism
CP-609754 是高效的、可逆的法尼基转移酶抑制剂,对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。
T36520 COR659

Cannabinoid Receptor; GABA Receptor GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。
T38294 4-Deoxypyridoxine hydrochloride

S1P Receptor GPCR/G Protein
4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解,与 S1P 一样,减少化学诱导的胰岛素瘤细胞系的细胞凋亡。
T36674 DMU-212

Apoptosis; ERK Apoptosis; MAPK
DMU-212 是具有口服活性的白藜芦醇的甲基化衍生物,表现出抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。它通过诱导凋亡和激活ERK1/2蛋白阻止有丝分裂。
T36949 Niaprazine

5-HT Receptor; Adrenergic Receptor; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Niaprazine 是有效的组胺 H1 受体拮抗剂,具有抗组胺和抗血清素活性。Niaprazine 在睡眠障碍方面有研究的价值。
T36968 ARN-21934

Topoisomerase DNA Damage/DNA Repair
ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂,具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM,ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。
T63474 RyRs activator 1

RyRs activator 1 是兰尼碱受体 (RyRs) 的有效激活剂。RyRs activator 1 在 0.5 mg/L 时,杀幼虫活性为100%,在 0.01 mg/L 时,杀幼虫活性为90%。
T28391 PF-9404C

PF9404C

PF-9404C is the S-S diesteroisomer of a beta adrenergic receptors blocker with vasodilatory properties. PF9404C increased the formation of cyclic GMP from 3 pmol mg1 protein in basal conditions, to 53 pmol mg1 protein in 10 μM in rat aorta smooth muscle
T38272 Thiacloprid

AChR; Parasite Microbiology/Virology; Neuroscience
Thiacloprid 属于氯烟碱类杀虫剂,主要用于防治蔬菜和果园中的蚜虫。它会破坏 DNA 的稳定性,通过疏水或氢相互作用,结合到小沟槽中,改变 DNA 的结构和稳定性。
T28245 ONO-0300302

ONO 0300302

ONO-0300302 is a slow tight binding LPA1 antagonist (IC50: 0.16 nM) used to treat Benign Prostatic Hyperplasia. ONO-0300302 inhibits significantly an LPA-induced increase of intraurethral pressure (IUP) in rat (3 mg/kg, p.o.) and dog (1 mg/kg, p.o.) over
T21968 MG-262

MG-262 是一种可逆的蛋白酶体抑制剂,具有多种生物活性。
T60949 Complex III-IN-2

Complex III-IN-2 (Compd 4d-2) 是complex III 的抑制剂,具有抗真菌活性,其对植物病菌立枯病菌和核盘菌的EC50值分别为29.31 mg/L 和 29.98 mg/L。
T37657 Mitochondrial respiration-IN-1 hydrobromide

Mitochondrial respiration-IN-1 hydrobromide (compound 49) is a potent mitochondrial inhibitor (IC50=8.8 mg/mL). Mitochondrial respiration-IN-1 hydrobromide significantly reduces mitochondrial respiration in platelets[1].
T70344 BJ-2302

BJ-2302 is a SRC inhibitor. BJ-2302 effectively suppressed MDA-MB-231 cell invasion (Matrigel invasion assay) and metastasis (chorioallantoic membrane assay xenografted with MDA-MB-231-luc2-tdTomato cancer cells). Additionally, BJ-2302 (1 mg/kg) strongly suppressed TNBC cell proliferation in vitro and tumor growth in a xenograft mouse tumor model. The anti-metastatic and anti-tumor effects of BJ-2302 were superior to those of Z-FL-COCHO (1 mg/kg) or batimastat (30 mg/kg), a pan-MMP inhibitor.
T81184 Sec61-IN-4

Sec61-IN-4(Compound 16b)作为Sec61抑制剂,其IC50值在U87-MG细胞中为0.04 nM。
T36599 4-Epianhydrotetracycline hydrochloride

Epianhydrotetracycline (EATC) is a degradation product of the antibiotic tetracycline .1 EATC is active against Pseudomonas, Agrobacterium, Moraxella, Bacillus, and E. coli (MIC50s = 0.75-16 mg/L).
T37286 1-Undecanoyl-rac-glycerol

1-Undecanoyl-rac-glycerol is a monoacylglycerol that contains undecanoic acid at the sn-1 position. It completely inhibits the growth of the bacteria B. cereus, B. subtilis, M. luteus, E. faecalis, and S. aureus when used at concentrations ranging from 250 to 1,500 mg/L.1 1-Undecanoyl-rac-glycerol (0.1 and 0.3 mg/ml) also has antifungal activity against K. marxianus, S. cerevisiae, and C. maltosa.2
T10462L Bavisant dihydrochloride hydrate

JNJ31001074AAC

Others Others
Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. in vivo: Mean change
T61009 Complex III-IN-1

Complex III-IN-1 (Compd 4c-2) 是 complex III 的抑制剂,具有抗真菌活性。Complex III-IN-1 对核盘菌的EC50值为 18.53 mg/L。
T82356 GABA-IN-1

GABA-IN-1 (Compound 6)为GABA抑制剂,具备显著的杀幼虫效能与杀虫功能,在浓度为50 mg/L时,致死率达93%。
T26610 AM-6761

AM 6761,AM6761

AM-6761 is a potent inhibitor of the MDM2-p53 interaction. In the SJSA-1 osteosarcoma xenograft model, AM-6761 shows excellent antitumor activity with an ED50 of 11 mg/kg.
T83067 Antifungal agent 81

Antifungalagent 81(G22) 对马利弧菌显示出显著的体外抑制活性,其IC50为0.48 mg/L。在体内,以40 mg/L的剂量,Antifungalagent 81同样展现出对马里弧菌的良好保护效果。
T7720 CGP 37849

CGP-37849,CGP37849

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
CGP 37849 是一种竞争性口服活性 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂((Ki = 35 nM)),具有有效性。CGP 37849 是啮齿动物的抗惊厥药,也具有抗抑郁和抗焦虑的特性。
T79399 E2730

GABA Receptor Membrane transporter/Ion channel; Neuroscience
E2730是一种针对γ-氨基丁酸(GABA)转运蛋白1(GAT1)的非竞争性选择性抑制剂,它能口服有效且有抗癫痫的作用。这种化合物能够随着环境中GABA水平的增加而增强其抑制GAT1的活性,从而有选择性地抑制GABA的回收。在实验模型中,E2730 (剂量范围为5-50 mg/kg; 经口给药) 在大鼠杏仁核点燃模型和小鼠的多种癫痫模型中,包括角膜点燃 (5-50 mg/kg)、耐药的6Hz-44mA精神运动癫痫 (5-50 mg/kg)、脆性X综合征 (2.5-300 mg/kg) 及Dravet综合征模型 (10 mg/kg, 20 mg/kg),展现了显著的体内活性。
T78804 PI3Kα-IN-12

PI3K PI3K/Akt/mTOR signaling
PI3Kα-IN-12(化合物13),作为一种高度选择性的PI3Kα抑制剂,展现出了1.2 nM的IC50值。在HCT-116和U87-MG细胞线上的抑制作用,IC50s分别为0.83 μM和1.25 μM。通过腹腔注射(IP)给予40 mg/kg的PI3Kα-IN-12,能够有效引起接受U87-MG细胞系异种移植的小鼠模型中的肿瘤退缩。
T79682 qsl-304

DNA/RNA Synthesis Cell Cycle/Checkpoint; DNA Damage/DNA Repair
QSL-304为一种DNA旋转酶B抑制剂,并具有抗菌作用,其对金黄色葡萄球菌sa-P2003的IC50值为31.23 mg/mL。
T81237 RyRs activator 4

RyRs activator 4为一款昆虫兰尼碱受体激活剂,对粘虫幼虫显示出显著的杀灭活性,其半致死浓度(LC50)为1.32 mg/L。
T61255 SDH-IN-1

SDH-IN-1 (compound 4i) is a potent succinate dehydrogenase (SDH) inhibitor, exhibiting an IC 50 value of 4.53 μM. This compound displays strong antifungal properties, particularly against S. sclerotiorum, with an EC 50 value of 0.14 mg/L [1].
T82834 Bombinin-BO1

Bombinin-BO1是一种蟾蜍皮肤分泌物中的抗菌肽,它对大肠杆菌(Escherichia coli)、金黄色葡萄球菌(Staphylococcus aureus)和白色念珠菌(Candida albicans)显示出抗生活性,其最小抑菌浓度(MIC)值分别为64 mg/L, 64 mg/L和128 mg/L。
T75279 Tigecycline tetramesylate

Tigecycline tetramesylate (GAR-936 tetramesylate)为一款广谱甘氨酰环素类抗生素,对E. coli (MG1655菌株)展现出约125 ng/mL的平均抑制浓度(MIC)。针对Acinetobacter baumannii (A. baumannii)的MIC50与MIC90分别达到1 mg/L与2 mg/L。
T79544 SDH-IN-6

SDH-IN-6 (compound 6i)是琥珀酸脱氢酶(SDH)的高效抑制剂,并显示出对Valsa mali的抗真菌活性,其EC50为1.77 mg/L。
T82355 GABA-IN-2

GABA-IN-2 (Compound 5) 为GABA抑制剂,展现出杀幼虫效果和显著的杀虫能力,在浓度50 mg/L下的死亡率达到87%。
T82835 Bombinin H-BO1

Bombinin H-BO1 是源自蟾蜍皮肤分泌物的抗菌肽,对白色念珠菌有效,其MIC值达256 mg/L。

化合物

MG 1
Cat.No: T12030
Synonym:
Target: Adrenergic Receptor
MG-101
Cat.No: T6583
Synonym: ALLN,Ac-LLnL-CHO,Calpain inhibitor I,Calpain inhibitor-1,MG101,钙蛋白酶抑制剂I
Target: Cysteine Protease, Proteasome
(R)-MG-132
Cat.No: T12628
Synonym: (S,R,S)-(-)-MG-132,N-[(苯基甲氧基)羰基]-L-亮氨酰-N-[(1S)-1-甲酰基-3-甲基丁基]-D-亮氨酰胺,Z-Leu-D-leu-leu-al
Target: Proteasome
Sitravatinib
Cat.No: T4349
Synonym: MG516,MGCD516
Target: Discoidin Domain Receptor (DDR), VEGFR, FLT, Trk receptor, TAM Receptor, c-Kit, Ephrin Receptor
N-Boc-4-pentyne-1-amine
Cat.No: T18391
Synonym:
Target: Others, PROTAC Linker
(S)-Vamicamide
Cat.No: T35033L
Synonym: (S)-Vamicamide (Iso-132373-81-0)
Target: AChE
MG-115
Cat.No: T21617
Synonym: Z-LL-Nva-CHO
Target: Proteasome
Eperezolid
Cat.No: T15237
Synonym: PNU-100592
Target: Antibacterial, Antibiotic
Tigecycline
Cat.No: T1569
Synonym: 替加环素,GAR-936
Target: ribosome, Antibacterial, Antibiotic, Autophagy
BIBB 515
Cat.No: T4039
Synonym:
Target: Others
KR-32568
Cat.No: T36569
Synonym:
Target: Sodium Channel
Litoxetine
Cat.No: T67956
Synonym:
Target: 5-HT Receptor
CS 2100
Cat.No: T22697
Synonym: 1-[[4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid
Target: S1P Receptor
RO1138452
Cat.No: T4436
Synonym: CAY10441
Target: Others, Prostaglandin Receptor
CCG-203971
Cat.No: T4306
Synonym: CCG203971
Target: Rho, Ras
Unifiram
Cat.No: T38192
Synonym:
Target: Others
MTP 131 acetate
Cat.No: T35689
Synonym:
Target: Others
CP-609754
Cat.No: T38050
Synonym:
Target: Transferase
COR659
Cat.No: T36520
Synonym:
Target: Cannabinoid Receptor, GABA Receptor
4-Deoxypyridoxine hydrochloride
Cat.No: T38294
Synonym:
Target: S1P Receptor
DMU-212
Cat.No: T36674
Synonym:
Target: Apoptosis, ERK
Niaprazine
Cat.No: T36949
Synonym:
Target: 5-HT Receptor, Adrenergic Receptor, Histamine Receptor
ARN-21934
Cat.No: T36968
Synonym:
Target: Topoisomerase
RyRs activator 1
Cat.No: T63474
Synonym:
Target:
PF-9404C
Cat.No: T28391
Synonym: PF9404C
Target:
Thiacloprid
Cat.No: T38272
Synonym:
Target: AChR, Parasite
ONO-0300302
Cat.No: T28245
Synonym: ONO 0300302
Target:
MG-262
Cat.No: T21968
Synonym:
Target:
Complex III-IN-2
Cat.No: T60949
Synonym:
Target:
Mitochondrial respiration-IN-1 hydrobromide
Cat.No: T37657
Synonym:
Target:
BJ-2302
Cat.No: T70344
Synonym:
Target:
Sec61-IN-4
Cat.No: T81184
Synonym:
Target:
4-Epianhydrotetracycline hydrochloride
Cat.No: T36599
Synonym:
Target:
1-Undecanoyl-rac-glycerol
Cat.No: T37286
Synonym:
Target:
Bavisant dihydrochloride hydrate
Cat.No: T10462L
Synonym: JNJ31001074AAC
Target: Others
Complex III-IN-1
Cat.No: T61009
Synonym:
Target:
GABA-IN-1
Cat.No: T82356
Synonym:
Target:
AM-6761
Cat.No: T26610
Synonym: AM 6761,AM6761
Target:
Antifungal agent 81
Cat.No: T83067
Synonym:
Target:
CGP 37849
Cat.No: T7720
Synonym: CGP-37849,CGP37849
Target: NMDAR, iGluR
E2730
Cat.No: T79399
Synonym:
Target: GABA Receptor
PI3Kα-IN-12
Cat.No: T78804
Synonym:
Target: PI3K
qsl-304
Cat.No: T79682
Synonym:
Target: DNA/RNA Synthesis
RyRs activator 4
Cat.No: T81237
Synonym:
Target:
SDH-IN-1
Cat.No: T61255
Synonym:
Target:
Bombinin-BO1
Cat.No: T82834
Synonym:
Target:
Tigecycline tetramesylate
Cat.No: T75279
Synonym:
Target:
SDH-IN-6
Cat.No: T79544
Synonym:
Target:
GABA-IN-2
Cat.No: T82355
Synonym:
Target:
Bombinin H-BO1
Cat.No: T82835
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6S2252 Sweroside

Others Others
Sweroside 是分离自Lonicera japonica 中,具有细胞保护、抗骨质疏松和保护肝脏活性。
T6S0033 Crotonoside

巴豆苷;异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE

Others; FLT; HDAC Angiogenesis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Others; Tyrosine Kinase/Adaptors
Crotonoside (Isoguanosine) 是从中草药巴豆中分离出来的一种天然产物。 它抑制 FLT3 和 HDAC3/6,有治疗急性髓性白血病 (AML)的研究潜力。
T2S0493 Isoeugenol

4-Propenylguaiacol,2-Methoxy-4-propenylphenol,异丁香酚,异丁香酚;4-丙烯基-2-甲氧基苯酚、对丙烯基邻甲氧基本酚、异丁子香酚

Antibacterial Microbiology/Virology
Isoeugenol (4-Propenylguaiacol) 是肉豆蔻,丁香和肉桂的精油成分,具有抗菌活性。它抑制Escherichia coli 和Listeria innocua,MIC 值分别为 0.6 mg/mL 和 1 mg/mL。
T5269 N-Acetylornithine

Acetyl-ornithine,N-Acetyl-L-ornithine,N-乙酰鸟氨酸

Others; Endogenous Metabolite Metabolism; Others
N-Acetylornithine (N-Acetyl-L-ornithine) 是一种人内源性代谢物,是 L-谷氨酸到 L-精氨酸的酶促合成中的中间体。
T5S1989 Apiin

Apioside,芹菜苷

Others Others
Apiin (Apioside) 是Apium graveolens 叶片的一种主要成分,具有抗炎作用。它在体外抑制亚硝酸盐产生的IC50值为0.08 mg/mL,在 LPS 激活的 J774.A1 细胞中抑制 iNOS 的表达的IC50值为0.049 mg/ mL。
T3868 Agnuside

牡荆油,穗花牡荆苷,chasteberry oil

COX; Prostaglandin Receptor; P-gp GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience
Agnuside (chasteberry oil) 是从黄荆中分离得到的一种天然产物,可下调炎性介质PGE2和LTB4,减少细胞因子的表达,具有抗关节炎活性。
T6S1141 Ganoderic acid A

灵芝酸 A,灵芝酸A

Apoptosis; NF-κB; Endogenous Metabolite; Autophagy Apoptosis; Autophagy; Metabolism; NF-κB
Ganoderic acid A 能够抑制 JAK-STAT3信号通路,也能抑制细胞增殖,存活率和 ROS。 它对人骨肉瘤 HOS 和MG-63细胞具有增殖抑制、凋亡和侵袭抑制作用。
TCS1704 Artemitin

艾黄素,Artemetin,Artemisetin,Erianthin

Antioxidant oxidation-reduction
Artemitin (Erianthin) 是一种存在于翼齿六棱菊中的天然黄酮,具有抗氧化、抗炎、抗病毒活性。
T4904 1-Methylguanidine hydrochloride

Others; Endogenous Metabolite Metabolism; Others
1-Methylguanidine hydrochloride 是内源性代谢产物的一种。
T4439 sn-Glycero-3-phosphocholine

Choline Alfoscerate,甘磷酸胆碱,Glycerophosphocholine,Glycerophosphorylcholine,Alpha-GPC,Choline glycerophosphate,L-α-GPC

Endogenous Metabolite; AChE Metabolism; Neuroscience
sn-Glycero-3-phosphocholine (Choline glycerophosphate) 是脑磷脂生物合成的前体,能够提高胆碱在神经组织中的生物利用度。它对认知功能有显著影响,同时具有良好的耐受性和安全性,因此能够用于阿尔茨海默病和痴呆症的研究。
T2776 Tribuloside

Tiliroside,刺蒺藜皂甙,蒺藜皂甙

Others; Antibacterial Microbiology/Virology; Others
Tribuloside (Tiliroside) A 是一种可从 Tribulus terrestris L 中分离得到的黄酮,可抑制非致病性分枝杆菌,MIC 值 为5.0 mg/mL。
TWS2045 Bruceine D

鸦胆子素D,鸦胆子苦素D

Apoptosis; Antiviral; Gamma-secretase; Parasite Apoptosis; Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome; Stem Cells
Bruceine D 是Notch 抑制剂,有抗癌活性,诱导几种人癌细胞调亡。它是一种有效的植物性昆虫拒食剂,有显著的系统特性和抑制害虫生长的作用。它具有较强的驱虫活性,抑制D. intermedius 的 EC50值为 0.57 mg/L。
T72742 (-)-Pinocembrin

(-)-乔松素

(-)-Pinocembrin 对 H37Ra 结核分枝杆菌展示了抗菌活性,无论是休眠还是活跃期,其 IC50 值分别为1.11 mg/mL 和 1.21 mg/mL。作为一种抗增殖剂,(-)-Pinocembrin 对于 THP-1、A549、Panc-1、HeLa 和 MCF7 细胞系,IC50 值范围为 1.88 至 11.00 mg/mL。
T83254 7,4'-Dihydroxyhomoisoflavane

7,4'-Dihydroxyhomoisoflavane 是一种具有抗氧化能力的天然化合物,能有效清除 ABTS 自由基,其半抑制浓度 (IC50) 为 0.22 mg/mL。
T79958 Isocrenatoside

Angiotensin-converting Enzyme (ACE) Metabolism
Isocrenatoside (compound 6)为环状八肽,具有ACE抑制活性。该化合物可通过乙醇提取Microtoena prainiana茎部分离纯化。研究显示,1 mg/mL浓度下,Isocrenatoside的ACE抑制效率高达99.3%。
T75701 8,3′,4′-Trihydroxyflavone-7-O-β-D-glucopyranoside

8,3′,4′-Trihydroxyflavone-7-O-β-D-glucopyranoside (Compound 3) 是一种可以从Bidens bipinnata 分离得到的天然产物。8,3′,4′-Trihydroxyflavone-7-O-β-D-glucopyranoside 在 0.556 mg/mL 时对α-amylase 有 22% 的抑制作用。
T37444 Aranorosin

Aranorosin is a fungal metabolite originally isolated from P. roseus. It has antimicrobial activity against B. subtilis, A. niger, and C. albicans when used at a concentration of 1 mg/ml. Aranorosin also reduces viability in apoptosis-resistant HeLa/Bcl-2 cells.
T83920 4-Trehalosamine

4-Trehalosamine是一种在Streptomyces中发现的微生物代谢产物,具有抗生素活性。在杯碟法测试中,当浓度为0.5、1和2 mg/ml时,对E. coli、K. pneumoniae和B. subtilis展现出活性。
T35532 Galegine hydrochloride

Galegine hydrochloride, a guanidine derivative derived from G. officinalis, plays a role in inducing weight loss in mice and has contributed to the development of biguanides, including metformin and phenformin. This compound stimulates AMPK activation in 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma, and HEK293 human kidney cell lines. Additionally, galegine hydrochloride exhibits antibacterial properties, particularly demonstrating a minimum inhibitory concentration of 4 mg/L against Staph...
T83903 Polymyxin B2 sulfate

Polymyxin B2是一种抗生素,并且是从B. polymyxa分离出的阳离子脂肽抗生素polymyxin B的主要成分。该化合物对P. aeruginosa、A. baumannii、K. pneumoniae和E. cloacae菌株具有活性(MICs分别为1-2、0.5-1、0.25-0.5和0.25-1 µg/ml)。在体内实验中,以4 mg/kg剂量的Polymyxin B2能显著降低P. aeruginosa血液感染小鼠模型中的血液集落形成单位(CFUs)数量。
T35624 Ajoene

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 &#181g/ml) and Gram-negative bacteria (MICs = 136-200 &#181g/ml), as well as yeasts (MICs = 10-20 &#181g/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 &#181M), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 &#181M).2It reduces...
T66078 Cardamonin

Cardamonin, a chalcone extracted from cardamom spice with anti-inflammatory and anti-tumor activities. Cardamonin decreased viability of NPC(Nasopharyngeal carcinoma ) cells in a concentration-dependent manner. The IC50 values were 16.22 μM(CNE-1), 14.34 μM (CNE-2), 16.50 μM (HONE-1), and 68.12 μM (SUNE-1). Moreover, the expression level of the proapoptotic effector protein Bax and Bid was also markedly increased after treatment with cardamonin(15μM) in CNE-2 cells.In vivo, cardamonin (25 mg/kg ...
T36179 Aspulvinone O

Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) redu...
T83915 Norbixin hydrate

Norbixin是一种在B. orellana中发现的类胡萝卜素,具有多样的生物活性。在无细胞测试中,它与过氧化物酶体增殖物激活受体γ (PPARγ)结合(Ki = 1.15 µM)。在心脑血管代谢综合征大鼠模型中,Norbixin (47.7 mg/kg) 能够减轻高血糖、高胰岛素血症和胰岛素抗性,降低血清脂质水平及心脏中硫代巴比妥酸反应性物质(TBARS)和谷胱甘肽(GSH)的水平。在胆固醇诱导的动脉粥样硬化兔模型中,它降低氧化型LDL和主动脉蛋白氧化水平,并减少动脉粥样硬化面积。Norbixin(每天0.11 mg/kg)减少汞诱导的大鼠肝细胞和白细胞DNA损伤。此外,它还能预防与年龄相关的黄斑变性(AMD)Abca4-/- Rdh8-/-小鼠模型中的光感受器退化。
T35752 Xanthoquinodin A1

Xanthoquinodin A1

Xanthoquinodin A1 is a fungal metabolite that has been found inHumicolaand has diverse biological activities.1,2It inhibitsE. tenellaschizont formation in BHK-21 cells with a minimum effective concentration (MEC) value of 0.02 μg/ml.1Xanthoquinodin A1 is active againstB. subtilis,M. luteus,S. aureus,A. laidlawii, andB. fragilisin a disc assay when used at a concentration of 1 mg/ml. It is also active againstB. cereus(MIC = 0.44 μM).2Xanthoquinodin A1 is cytotoxic to KB, MCF-7, and NCI H187 cance...
T35750 Trypacidin

Trypacidin is a fungal metabolite originally isolated fromA. fumigatus.1It is active againstB. subtilisandM. bovis(MICs = 12.5 and 1.25 μg/ml, respectively), as well asT. cruziandT. gondii(MICs = 5-10 and 10-20 μg/ml, respectively).1,2It reduces viability and induces lysis of A549 human lung cancer cells (IC50s = 7.4 μM for both).3Trypacidin increases survival in a mouse model ofT. gondiiinfection when administered in six doses of 12.5 mg/kg each.1 1.Balan, J., Ebringer, L., Nemec, P., et al.Ant...
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...
T36227 Beauveriolide III

Beauveriolide III is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.41 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide III also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 5.5 μM).2Beauveriolide III (25 and 50 mg/kg) reduces the size of aortic ...
T35751 Violacein

Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 &#181M, respectively). It is also active aga...
T35779 Oosporein

Oosporein is a mycotoxin that has been found inBeauveriaand has diverse biological activities.1,2It is cytotoxic to Sf9 and Sf21 insect cells with 50% cytotoxic concentration (CC50) values of 4.23 and 10.43 μM, respectively.3Oosporin induces lethality in day-old cockerels (LD50= 6.12 mg/kg).4It inhibits Na+/K+-, Ca2+-, and Mg2+-ATPase activities by 27, 52, and 100%, respectively, in equine erythrocyte ghosts when used at a concentration of 200 μg/ml.2Oosporein inhibits herpes simplex 1 (HSV-1), ...
T36448 (E)-Ajoene

(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanoth...
T36954 Nemorosone

Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nem...

天然产物

Sweroside
Cat.No: T6S2252
Synonym:
Target: Others
Crotonoside
Cat.No: T6S0033
Synonym: 巴豆苷;异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE
Target: Others, FLT, HDAC
Isoeugenol
Cat.No: T2S0493
Synonym: 4-Propenylguaiacol,2-Methoxy-4-propenylphenol,异丁香酚,异丁香酚;4-丙烯基-2-甲氧基苯酚、对丙烯基邻甲氧基本酚、异丁子香酚
Target: Antibacterial
N-Acetylornithine
Cat.No: T5269
Synonym: Acetyl-ornithine,N-Acetyl-L-ornithine,N-乙酰鸟氨酸
Target: Others, Endogenous Metabolite
Apiin
Cat.No: T5S1989
Synonym: Apioside,芹菜苷
Target: Others
Agnuside
Cat.No: T3868
Synonym: 牡荆油,穗花牡荆苷,chasteberry oil
Target: COX, Prostaglandin Receptor, P-gp
Ganoderic acid A
Cat.No: T6S1141
Synonym: 灵芝酸 A,灵芝酸A
Target: Apoptosis, NF-κB, Endogenous Metabolite, Autophagy
Artemitin
Cat.No: TCS1704
Synonym: 艾黄素,Artemetin,Artemisetin,Erianthin
Target: Antioxidant
1-Methylguanidine hydrochloride
Cat.No: T4904
Synonym:
Target: Others, Endogenous Metabolite
sn-Glycero-3-phosphocholine
Cat.No: T4439
Synonym: Choline Alfoscerate,甘磷酸胆碱,Glycerophosphocholine,Glycerophosphorylcholine,Alpha-GPC,Choline glycerophosphate,L-α-GPC
Target: Endogenous Metabolite, AChE
Tribuloside
Cat.No: T2776
Synonym: Tiliroside,刺蒺藜皂甙,蒺藜皂甙
Target: Others, Antibacterial
Bruceine D
Cat.No: TWS2045
Synonym: 鸦胆子素D,鸦胆子苦素D
Target: Apoptosis, Antiviral, Gamma-secretase, Parasite
(-)-Pinocembrin
Cat.No: T72742
Synonym: (-)-乔松素
Target:
7,4'-Dihydroxyhomoisoflavane
Cat.No: T83254
Synonym:
Target:
Isocrenatoside
Cat.No: T79958
Synonym:
Target: Angiotensin-converting Enzyme (ACE)
8,3′,4′-Trihydroxyflavone-7-O-β-D-glucopyranoside
Cat.No: T75701
Synonym:
Target:
Aranorosin
Cat.No: T37444
Synonym:
Target:
4-Trehalosamine
Cat.No: T83920
Synonym:
Target:
Galegine hydrochloride
Cat.No: T35532
Synonym:
Target:
Polymyxin B2 sulfate
Cat.No: T83903
Synonym:
Target:
Ajoene
Cat.No: T35624
Synonym:
Target:
Cardamonin
Cat.No: T66078
Synonym:
Target:
Aspulvinone O
Cat.No: T36179
Synonym:
Target:
Norbixin hydrate
Cat.No: T83915
Synonym:
Target:
Xanthoquinodin A1
Cat.No: T35752
Synonym: Xanthoquinodin A1
Target:
Trypacidin
Cat.No: T35750
Synonym:
Target:
(rel)-Asperparaline A
Cat.No: T37609
Synonym:
Target:
Beauveriolide III
Cat.No: T36227
Synonym:
Target:
Violacein
Cat.No: T35751
Synonym:
Target:
Oosporein
Cat.No: T35779
Synonym:
Target:
(E)-Ajoene
Cat.No: T36448
Synonym:
Target:
Nemorosone
Cat.No: T36954
Synonym:
Target:
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