XP-524
Published date: 2022-06-22 21:57:40
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Name | XP-524 | CAS# | 2344825-52-9 |
|---|---|---|---|---|
| Price | $Inquiry/100mg $Inquiry/250mg $Inquiry/1g | Purity | 98.0% | |
| Stocking Period |
3 Day | Stock | 3 | |
| Product Webpage: | https://www.dcchemicals.com/product_show-xp-524.html | |||
| Detail
Product Information
XP-524 (XL-223, XP524) is a potent, dual-BET/EP300 inhibitor, inhibits BRD4-BD (IC50=5.8 nM) and BRD4-BD2 (IC50=1.5 nM).XP-524 binds strongly to and inhibits EP300 and CBP proteins with IC50 of 28 and 116 nM, respectively.XP-524 (XL-223) showed high potency and selectivity (Kd 400-fold.XP-524 significantly decreased expression of Myc pathway oncogenes such as c-MYC and n-MYC, increased expression of CDKN1B, a tumor suppressor that prevents the activation of the cyclin-D/CDK4 complex, and also reduced expression of cyclin-D (CCND1) itself.XP-524 showed increased potency and superior tumoricidal activity than the benchmark BET inhibitor JQ-1 in vitro, with comparable efficacy to higher-dose JQ-1 combined with the EP300/CBP inhibitor SGC-CBP30.XP-524 prevented KRAS-induced, neoplastic transformation in vivo and extended survival in two transgenic mouse models of aggressive PDAC. |
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