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9

抑制剂 & 化合物

6

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9880 ZINC05007751

MAPK MAPK
ZINC05007751 是 NIMA 相关激酶 NEK6 的有效抑制剂(IC50 = 3.4 μM)。 ZINC05007751 对 NEK1 和 NEK6 具有很强的特异性,对 NEK2、NEK7 和 NEK9 没有显着的活性。
T5858 Sertindole

Lu 23-174,舍吲哚

Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Autophagy Autophagy; GPCR/G Protein; Neuroscience
Sertindole (Lu 23-174) 是一种非典型抗精神病药,可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合,Kd 值分别为 2.7、20、0.14 和 6 nM。
T7337 Kinetin riboside

N6-Furfuryladenosine,动力精核苷

Apoptosis Apoptosis
Kinetin riboside (N6-Furfuryladenosine) 是一种细胞分裂素类似物,可诱导癌细胞凋亡, 抑制 HCT-15 细胞的增殖,IC50 为 2.5 μM。
T61827 RJ-34

RJ-34, an aristolactam analogue, demonstrates strong antitumor effects across a wide range of cancer cell lines, with subnanomolar GI 50 values (GI 50 <0.1 nM) observed for A431, MES-SA, MES-SA/DX5, HCT-15, and HCT-15/CLO2 cells [1].
T79451 WES-1

Carbonic Anhydrase Metabolism
WES-1(Compound 8g)是一种针对碳酸酐酶IX的抑制剂,其抑制常数(Ki)为55.9 μM。该化合物对包括白血病细胞系(K-562、MOLT-4)、非小细胞肺癌(NCI-H460)、结肠癌(HCT 116、HCT-15)以及黑色素瘤(LOX IMVI)在内的多种癌细胞表现出抗增殖效果。
T74627 Angiogenesis inhibitor 3

Angiogenesis inhibitor 3 (compound 8) 是一种有效的血管生成(angiogenesis)抑制剂,能够抑制HUVEC和HCT-15细胞增殖,其IC50值分别为1.00和0.71 μM。此外,此化合物还能诱导这两种细胞的凋亡(apoptosis)并具有抑制癌细胞侵袭的抗癌活性。Angiogenesis inhibitor 3还能够抑制斑马鱼胚胎的血管生成。
T83887 SLU-10482

SLU-10482是一种抗寄生虫化合物,能减少HCT-8细胞中C. parvum寄生虫的数量(EC50 = 0.07 µM)。相较于另一种抗寄生虫化合物SLU-2633,SLU-10482与人类ether-a-go-go (hERG; Kd = 43 µM)的结合能力较弱。在体内,SLU-10482以5和15 mg/kg的剂量,每天两次给药,能减少C. parvum感染小鼠模型中粪便中卵囊的数量。
T68480 4SC-207

4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome a...
T36782 TAK1-IN-2

TAK1-IN-2

TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM[1]. TAK1-IN-2 (compound 54) (10 μM) has no effect on cell viability in TNF-α stimulated HCT-15 cells[1]. [1]. Veerman JJN, et, al. Discovery of 2,4-1 H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562.

化合物

ZINC05007751
Cat.No: T9880
Synonym:
Target: MAPK
Sertindole
Cat.No: T5858
Synonym: Lu 23-174,舍吲哚
Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, Autophagy
Kinetin riboside
Cat.No: T7337
Synonym: N6-Furfuryladenosine,动力精核苷
Target: Apoptosis
RJ-34
Cat.No: T61827
Synonym:
Target:
WES-1
Cat.No: T79451
Synonym:
Target: Carbonic Anhydrase
Angiogenesis inhibitor 3
Cat.No: T74627
Synonym:
Target:
SLU-10482
Cat.No: T83887
Synonym:
Target:
4SC-207
Cat.No: T68480
Synonym:
Target:
TAK1-IN-2
Cat.No: T36782
Synonym: TAK1-IN-2
Target:
Cat. No. Product Name Target Signaling Pathways
TN1516 Cnidicin

蛇床素,4,9-双[(3-甲基-2-丁烯-1-基)氧基]-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮

NOS; NO Synthase Immunology/Inflammation
Cnidicin 是一种香豆素,对肥大细胞脱颗粒及 RAW 264.7 细胞产生一氧化氮具有抑制作用。
TN3235 7-Hydroxycadalene

5-HT Receptor GPCR/G Protein; Neuroscience
7-Hydroxycadalene shows cytotoxicity activity against HCT-15 cell line with IC50 18.89 ± 1.2 uM.
TN3686 Coccinic acid

Others Others
Coccinic acid shows inhibitory effects against colorectal carcinoma HCT-15 and oral epithelial cell line KB-3-1.Mixture of coccinic acid and anwuweizonic acid shows significant inhibitory activity against human decidual cells and rat luteal cells in vitro
TN6014 Norcepharadione B

鱼腥草

Norcepharadione B shows good inhibitory activity against the replication of HSV-1, it also shows antimalarial activity with EC50 values of 7.5mug/ml. Norcepharadione B exhibits significant cytotoxicity against five human tumor cell lines (A-549, SK-OV-3,
TN4959 Schizandriside

Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation
Schizandriside may have anti-inflammatory effects, it has inhibitory activities against nitric oxide and prostaglandin E(2) production in IFN-γ- and lipopolysaccharide-stimulated RAW 264.7 cells. It shows significant cytotoxicity against A549, SK-OV-3, SK
TN2977 3-O-trans-p-Coumaroyltormentic acid

Caspase; Antifection Apoptosis; Microbiology/Virology; Proteases/Proteasome
3-O-(E)-p-coumaroyl tormentic acid may be promising lead compound for developing an effective drug for treatment of leukemia, it induces apoptotic cell death in human leukemia (HL60) via mainly mitochondrial pathway by, at least in part, Topo I inhibition. 3-O-trans-p-coumaroyltormentic acid shows cytotoxicity against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) in vitro, the IC50 values of 13.72, 14.29,14.61, 14.04 uM, respectively. 3beta-O-cis-p-Coumaroyltormentic acid, an...

天然产物

Cnidicin
Cat.No: TN1516
Synonym: 蛇床素,4,9-双[(3-甲基-2-丁烯-1-基)氧基]-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮
Target: NOS, NO Synthase
7-Hydroxycadalene
Cat.No: TN3235
Synonym:
Target: 5-HT Receptor
Coccinic acid
Cat.No: TN3686
Synonym:
Target: Others
Norcepharadione B
Cat.No: TN6014
Synonym: 鱼腥草
Target:
Schizandriside
Cat.No: TN4959
Synonym:
Target: Prostaglandin Receptor
3-O-trans-p-Coumaroyltormentic acid
Cat.No: TN2977
Synonym:
Target: Caspase, Antifection
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