VPC-14228
CAS No. : 19983-28-9
| Size | Price | Stock |
|---|---|---|
| 5mg | $110 | In-stock |
| 10mg | $180 | In-stock |
| 25mg | $380 | In-stock |
| 50mg | $600 | In-stock |
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| Cat. No. : | HY-117669 |
| M.Wt: | 246.33 |
| Formula: | C13H14N2OS |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
VPC-14228 is an inhibitor that selectively targets androgen receptor DNA binding domain (AR-DBD). VPC-14228 inhibits the interaction between AR and DNA, thereby blocking AR-mediated transcriptional activation. VPC-14228 does not rely on nuclear localization inhibition, but rather inhibits the activity of full-length AR and splice variant AR-V7 by interfering with AR binding to chromatin. And VPC-14228 has high selectivity for other nuclear receptors such as ER and PR. VPC-14228 can be used in the study of prostate cancer[1].
In Vitro:VPC-14228 inhibits hAR transcriptional activity in PC3 cells by targeting AR-DBD, with IC50s of 2.36 μM (hAR-WT), 3.70 μM (hAR-Y594A), and 3.70 μM (hAR-Q592A) for hAR[1].
VPC-14228 (25 μM; 6 h) did not induce apoptosis or affect AR protein expression[1].
VPC-14228 may degrade AR-V7 in 22Rv1 cells via VHL-like PROTACs, but has no effect at 10 μM concentration[2].
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