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

Chemical Structure : COUP-TFII inhibitor CIA1

COUP-TFII inhibitor CIA1 (CIA1)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt	365.876
Formula	C17H20ClN3O2S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(3,4-dimethoxyphenethyl)-6-methylthieno[2,3-d]pyrimidin-4-amine hydrochloride

References

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

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COUP-TFII inhibitor CIA1 (CIA1)

Biological Activity

Physicochemical Properties

References

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