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SU9516

CDKs的选择性有效ATP竞争性抑制剂
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货号 (SKU) 包装规格 是否现货 价格 数量
S336668-5mg
 5mg 期货 Stock Image
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cyclin dependent kinase 1 Inhibitor cyclin dependent kinase 2 Inhibitor cyclin dependent kinase 4 Inhibitor cyclin dependent kinase 5 Inhibitor cyclin dependent kinase 7 Inhibitor cyclin dependent kinase 9 Inhibitor
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基本描述

英文名称 SU9516
英文别名 (Z)-3-((1H-imidazol-5-yl)methylene)-5-methoxyindolin-2-one
储存温度 2-8°C储存
运输条件 冰袋运输
产品介绍

SU9516是在肿瘤细胞中表现出抗增殖和促凋亡特性的3-取代的吲哚满酮化合物。SU9516显示出作为CDK的选择性强效ATP竞争性抑制剂的活性。它还对PKC，p38，PDGFRβ或EGFR的活性无明显影响（IC | 50 |> 10μM）。SU9516通过与Cdk2结合并阻止pRb的磷酸化及其从E2F的解离，对生长因子刺激的结肠癌细胞的增殖具有抑制作用。SU9516是Cdc2，Cdk2和Cdk4的抑制剂。

SU9516 is a 3-substituted indolinone compound displaying anti-proliferative and proapoptotic properties in tumor cells. SU9516 displays activity as a selectively potent ATP-competitive inhibitor of CDKs. It also shows no significant effect (IC|50|>10 μM) on the activities of PKC, p38, PDGFRβ, or EGFR. SU9516 has an Inhibitory effect on proliferation of growth-factor stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F. SU9516 is an inhibitor of Cdc2, Cdk2 and Cdk4.

产品属性

pKa值 pK?: 12.20, pK?: 4.74
IC50 Cdk2/A: IC??= 22 nM; Cdk1/B: IC??= 40 nM; Cdk4/D1: IC??= 200 nM; PKC: IC??= >10 μM ; p38: IC??= >10 μM ; PDGFR: IC??= 18 μM ; EGFR : IC??= >100 μM ; ATP-dependent molecular chaperone HSP82: EC5050 = 1250 nM (Candida albIC??s ); Trypanosoma brucei: EC5050

名称和标识符

IUPAC Name 3-(1H-imidazol-5-ylmethylidene)-5-methoxy-1H-indol-2-one
INCHI InChI=1S/C13H11N3O2/c1-18-9-2-3-12-10(5-9)11(13(17)16-12)4-8-6-14-7-15-8/h2-7H,1H3,(H,14,15)(H,16,17)
InChi Key QNUKRWAIZMBVCU-UHFFFAOYSA-N
Canonical SMILES COC1=CC2=C(C=C1)NC(=O)C2=CC3=CN=CN3
WGK Germany 3
PubChem CID 24906268
分子量 241.25

化学和物理性质

溶解性 Soluble in DMSO (10 mg/ml), and ethanol (20 mM). Insoluble in water.
密度 1.38 g/cm3(Predicted)
折光率 n20D1.70 (Predicted)
沸点 601.52° C at 760 mmHg (Predicted)
熔点 220.28° C (Predicted)

安全和危险性（GHS）

WGK Germany 3

关联配体

Ligand ID 6045
名称 SU9516
别名 AC1NRD9P
类别 Synthetic organic
学名 (3Z)-3-(1H-imidazol-5-ylmethylidene)-5-methoxy-2,3-dihydro-1H-indol-2-one
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 SU9516 is a potent inhibitor of several cyclin-dependent kinases (CDKs) with reported selectivity for CDK2 . Later analysis of SU9516's selectivity profile indicates a similar level of potency as an inhibitor of CDK5/p25 compared to CDK2 . Inhibition of CDK5 was confirmed in a cellular assay measuring dephosphorylation of pFAK(S732). SU9516 also arrests cells at the G2/M phase in cells lacking CDK2, in which case it must be causing the cell cycle arrest via inhibition of CDK1 .

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参考文献

1. Lane ME, Yu B, Rice A, Lipson KE, Liang C, Sun L, Tang C, McMahon G, Pestell RG, Wadler S.  (2001)  A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells..  Cancer Res,  61  (16):  (6170-7).  [PMID:11507069]
2. Jorda R, Hendrychová D, Voller J, ?ezní?ková E, Gucky T, Kry?tof V.  (2018)  How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?.  J Med Chem,  61  (20):  (9105-9120).  [PMID:30234987]
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