COUP-TFII inhibitor CIA1 |CAS:1049691-47-5 Probechem Biochemicals

Chemical Structure : COUP-TFII inhibitor CIA1

CAS No.: 1049691-47-5

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COUP-TFII inhibitor CIA1 (CIA1)

货号: PC-38207Not For Human Use, Lab Use Only.

CIA1 (COUP-TFII inhibitor A1) is a potent and specific inhibitor of COUP-TFII activity, inhibits COUP-TFII–driven NGFIA reporter expression with IC50 of 3.2 uM, disturbs COUP-TFII binding to FOXA1 to regulate target gene expression.

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25 mg	￥1580	In stock
50 mg	￥2580	In stock
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生物&药学活性

CIA1 (COUP-TFII inhibitor A1) is a potent and specific inhibitor of COUP-TFII activity, inhibits COUP-TFII–driven NGFIA reporter expression with IC50 of 3.2 uM, disturbs COUP-TFII binding to FOXA1 to regulate target gene expression.

CIA1 repressed NGFIA reporter expression in a COUP-TFII–dependent manner, as COUP-TFII knockdown abrogated CIA1-induced inhibition.

CIA1 directly interacts with COUP-TFII protein, CIA1 treatment resulted in a thermal stabilization of COUP-TFII.

CIA1 inhibited growth of multiple prostate cancer cell lines including androgen-sensitive LNCaP cells, AR-negative PC3 cells, as well as CRPC C4-2, abl, and AR variant 22Rv1 cells with IC50 of 1.2 to 7.6 uM, also notably inhibited the colony formation ability of prostate cancer cells in a dose-dependent manner.

COUP-TFII inhibitor CIA1 can phenocopy COUP-TFII silencing, with no apparent effect COUP-TFII protein levels, disturbed COUP-TFII target genes in tumor samples, including induced FOXM1, CDK1, and repressed p21.

COUP-TFII inhibitor CIA1 (2.6 mg/kg, i.p.) inhibited prostate cancer tumor growth in PC3 xenograft in the mice that bear PC3 xenograft, with limited toxicity.

物理化学性质&存储条件

分子量	365.876
分子式	C17H20ClN3O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(3,4-dimethoxyphenethyl)-6-methylthieno[2,3-d]pyrimidin-4-amine hydrochloride

参考文献

1. Leiming Wang, et al. Sci Adv. 2020 Apr 29;6(18):eaaz8031.

COUP-TFII inhibitor CIA1 (CIA1)

生物&药学活性

物理化学性质&存储条件

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COUP-TFII inhibitor CIA1 (CIA1)

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物理化学性质&存储条件

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