ZXH-3-26
CAS No. : 2243076-67-5
| Size | Price | Stock |
|---|---|---|
| 5mg | $396 | In-stock |
| 10mg | $649 | In-stock |
| 50mg | $2090 | In-stock |
| 100mg | $3190 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-122826 |
| M.Wt: | 785.27 |
| Formula: | C38H37ClN8O7S |
| Purity: | >98 % |
| Solubility: | DMSO : 200 mg/mL (ultrasonic) |
ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM[1].
In Vitro: ZXH-3-26 represents the first small molecule to allow pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2/3[1].
ZXH-3-26 shows activity exclusively on the first bromodomain of BRD4, and spares degradation of BRD2/3 at concentrations 10 μM. Immunoblot analysis confirms that ZXH-3-26 degrades endogenous BRD4 with comparable efficacy compared to the best pan-BET degrader dBET6, while being inactive on BRD2/3[1].
ZXH-3-26 engages CRBN in a conformation distinct[1].
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