Cdc 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S7547 XL413 (BMS-863233)

XL413 (BMS-863233) 是强效的选择性的cell division cycle 7 homolog (CDC7) kinase抑制剂,IC50为3.4 nM,其选择性分别超过 CK2, Pim-1 和pMCM2选择性的 63-, 12-和35-倍。 Phase 1/2。

Selective Cdc7, IC50: 3.4 nM
S6777 NSC95397

NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor with Ki of 32 nM, 96 nM, 40 nM for Cdc25A, Cdc25B and Cdc25C, respectively. NSC 95397 has IC50 of 22.3 nM, 56.9 nM and 125 nM for human Cdc25A, human Cdc25C and Cdc25B, respectively. NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.

Selective Cdc25C, IC50: 125 nM; Cdc25B, IC50: 56.9 nM; Cdc25A, IC50: 22.3 nM; Cdc25C, Ki: 40 nM; Cdc25B, Ki: 96 nM; Cdc25A, Ki: 32 nM
S6540 NG 52

NG-52 is a tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p with IC50s of 7 and 2 μM, respectively.

Selective Pho85p, IC50: 2 μM; Cdc28p, IC50: 7 μM
S9650 LY3143921 hydrate

LY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor.

S9605 Apcin

Apcin is an anaphase-promoting complex/cyclosome (APC/C) inhibitor. Apcin blocks mitotic exit and is synergistically amplified by co-addition of Ts-Arg-OMe.

S7793 Purvalanol A

Purvalanol A 是一种有效的,细胞渗透性 CDK 抑制剂,对cdc2-cyclin B,cdk2-cyclin A,cdk2-cyclin E,和 cdk4-cyclin D1的 IC50 分别为 4 nM,70 nM,35 nM,和 850 nM。

Pan Cdc2/CyclinB, IC50: 4 nM
S0500 Purvalanol B

Purvalanol B (NG-95) is an inhibitor of cyclin-dependent kinase with IC50 of 6 nM, 6 nM, 9 nM, > 10,000 nM and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35, respectively.

Pan cdc2-cyclin B, IC50: 6 nM
S2742 PHA-767491

PHA-767491是一种有效的,ATP竞争性的,双重Cdc7/CDK9抑制剂,无细胞试验中IC50分别为10 nM和34 nM,比作用于CDK1/2和GSK3-β选择性高20倍左右,比作用于MK2和CDK5选择性高50倍,比作用于PLK1和CHK2选择性高100倍。

Pan Cdc7, IC50: 10 nM
S1153 Roscovitine (CYC202)

Roscovitine (Seliciclib,CYC202)是一种有效的,选择性CDK抑制剂,作用于Cdc2CDK2CDK5时,无细胞试验中IC50分别为0.65 μM,0.7 μM和0.16 μM,对CDK4/6几乎没有作用。Phase 2。

Pan Cdc2/CyclinB, IC50: 0.65 μM
S3224 Cinobufagin

Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.