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ABC1183

ABC1183是一种抑制GSK3α， GSK3β和CDK9的新型二氨基噻唑。ABC1183通过诱导G2/M 阻滞和改变GSK3、糖原合成酶、β-catenin 磷酸化和MCL1表达降低细胞存活率来抑制多种癌细胞株的生长，并具有口服活性。

CAS号

1042735-18-1

分子式

C18H14N4OS

主要靶点

CDK|GSK-3

仅限科研使用

Cat No : CM09616

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Synonyms

ABC 1183|ABC-1183

验证数据展示

  • CAS No.: 1042735-18-1

    ABC1183
    CAS#: 1042735-18-1

产品信息

ABC1183 is a novel diaminothiazole that inhibits GSK3α, GSK3β and CDK9. ABC1183 inhibits the growth of a numerous cancer cell lines by decreasing cell survival by inducing G2/M arrest and through altering GSK3, glycogen synthetase, β-catenin phosphorylation and MCL1 expression,and is orally active.

CAS号 1042735-18-1
分子式 C18H14N4OS
主要靶点 CDK|GSK-3
主要通路 细胞周期|PI3K/Akt/mTOR信号通路|干细胞
分子量 334.4
纯度 98.53%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 ABC 1183|ABC-1183

靶点活性

CDK9/cyclin T1:321 nM|GSK3α:327 nM|GSK3β:657 nM

体内活性

Murine melanoma B16 tumors were propagated in C57BL/6 mice were treated with oral ABC1183 or vehicle. Tumor growth was decreased more than 70% within 8 days by ABC1183 treatment. On the basis of body weight, gross toxicities were not observed. ABC1183 was determined to suppress tumor growth in the absence of organ and hematopoietic toxicity. The expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) were suppressed[1][2].

体外活性

ABC1183 inhibits cell proliferation and tumor growth of various cancer types by specifically attenuating GSK3 and CDK9 activity. ABC1183 altered GSK3 activity as indicated by decreased GSK3α/β and GS phosphorylation and increased β-catenin phosphorylation[1].

溶解度

DMSO:3.34 mg/mL (10 mM),Sonification is recommended.

参考文献

1.Schrecengost RS, et al. In Vitro and In Vivo Antitumor and Anti-Inflammatory Capabilities of the Novel GSK3 and CDK9 Inhibitor ABC1183. J Pharmacol Exp Ther. 2018 Apr;365(1):107-116.
2.Duda P, et al. Targeting GSK3 and Associated Signaling Pathways Involved in Cancer. Cells. 2020 Apr 30;9(5):1110.

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