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CHIR-124

CAS No. : 405168-58-3

MCE 站：CHIR-124

产品活性：CHIR-124 是一种有效的，选择性的 Chk1 抑制剂，IC₅₀ 值为 0.3 nM；同时可有效抑制 PDGFR 和 FLT3，IC₅₀ 值分别为 6.6 nM 和 5.8 nM。

研究领域：Cell Cycle/DNA Damage  |  Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：Checkpoint Kinase (Chk)  |  FLT3  |  PDGFR  |  Apoptosis

In Vitro: CHIR-124 is 500- to 5,000-fold less active against other cell cycle kinases, such as cyclin-dependent kinase 2/cyclin A (0.19 μM), cdc2/cyclin B (0.51 μM), and cyclin-dependent kinase 4/cyclin D (2.1 μM). CHIR-124 (≥0.9 nM) in combination with SN-38 (≥0.42 nM) causes significant synergy or >10% deviation from additivity in human cancer cell lines expressing mutant p53, and these values overlap and fall below the IC₅₀s for SN-38 (1.2×10^-7 M) and CHIR-124 (2.2×10^-7 M), respectively. Moreover, CHIR-124 (100 nM) abrogates the SN-38-induced S and G2-M phase cell cycle checkpoints. CHIR-124 (200 nM) leads to a 2.5-fold elevated level of cdc25A above that of the untreated HCT116 p53^?/? cells. The down-regulation of cdc25A induced by SN-38 is completely restored by concurrent or sequential treatment with CHIR-124, proving that CHIR-124 inhibits the Chk1-mediated destruction of cdc25A in whole cells. CHIR-124 occupies the ATP-binding site, inhibits Chk1 (IC₅₀, 0.3 nM) 2,000-fold more potently than Chk2 (IC₅₀, 0.7 μM).

In Vivo: CHIR-124 (10 or 20 mg/kg, p.o.) does not have a significant effect on tumor growth when compared with the vehicle-treated group, but it potentiates the growth inhibitory effect of CPT-11 in a human breast carcinoma xenograft model. The potentiation of the tumor growth inhibitory effect of CPT-11 by CHIR-124 is associated with an increase in apoptosis induction in the tumors. CHIR-124 reverses the suppression of phospho-H3 staining induced by CPT-11, indicating abrogation of the G2-M checkpoint by CHIR-124.

相关产品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Reprogramming Compound Library  |  Anti-Blood Cancer Compound Library  |  MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Y-27632 dihydrochloride  |  Acetylcysteine  |  Angiotensin II human  |  SP600125  |  5-Fluorouracil  |  Staurosporine  |  Bortezomib  |  Tamoxifen  |  2-Deoxy-D-glucose  |  Gemcitabine  |  Verteporfin  |  Decitabine  |  Actinomycin D  |  Temozolomide  |  BAY 11-7082  |  Etoposide  |  Mitomycin C  |  CCCP  |  DAPT  |  Rote  |  Etomoxir  |  Stattic  |  Docetaxel  |  Fulvestrant

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