GEM144

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GEM144 

GEM144 是一种有效且具有口服活性的 DNA polymerase α (POLA1) 和 HDAC 11 双重抑制剂。GEM144 诱导 p53 乙酰化、激活 p21、G1/S 细胞周期阻滞和细胞凋亡 (apoptosis)。

GEM144

GEM144 Chemical Structure

CAS No. : 2487526-28-1

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生物活性

GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts[1].

IC50 & Target

HDAC11

8.23 μM (IC50)

体外研究
(In Vitro)

GEM144 (0-10 μM; 24 hours) exhibits antiproliferative activity in tested cancer cell lines with IC50s of 0.26 ~ 2.2 μM[1].
GEM144 (0.1 – 0.4 μM; 24 hours) strongly increases levels of H2AX phosphorylation on Ser 39 (γH2AX), and strongly upregulates p21 expression in a dose-dependent manner[1].
GEM144 (0.26 μM in NCI-H4609, 0.95 μM in A2780 and 1.4 μM in MM473; 72 hours) induced G1/S cell cycle arrest[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: NCI-H460, H460-R9A, A2780 and A2780-DX[1]
Concentration: 0-10 μM
Incubation Time: 24 hours (further 48 h growth in drug-free medium)
Result: Exhibited antiproliferative activity in tested cancer cell lines with IC50s of 0.26 ~ 2.2 μM.

Western Blot Analysis

Cell Line: NCI-H460[1]
Concentration: 0.1 μM, 0.25 μM and 0.4 μM
Incubation Time: 24 hours
Result: Strongly increased levels of H2AX phosphorylation on Ser 39 (γH2AX), and strongly upregulated p21 expression in a dose-dependent manner.

Cell Cycle Analysis

Cell Line: NCI-H4609, A2780 and MM473[1]
Concentration: 0.26 μM in NCI-H4609, 0.95 μM in A2780 and 1.4 μM in MM473
Incubation Time: 72 hours
Result: Induced G1/S cell cycle arrest.

体内研究
(In Vivo)

GEM144 (50 mg/kg; p.o., bid, 5 days a week, for 3-4 weeks) significantly reduces tumor burden of MM487 with TGI of 72% in xenografts mice[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female CD-1 nude mice (injected with MM473 and MM487)[1]
Dosage: 50 mg/kg
Administration: PO, bid, 5 days a week, for 3-4 weeks
Result: Significantly reduced tumor burden of MM487 with TGI of 72%.

分子量

461.55

Formula

C28H31NO5
CAS 号

2487526-28-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Dallavalle S, et al. Antitumor activity of novel POLA1-HDAC11 dual inhibitors. Eur J Med Chem. 2022;228:113971.

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