(S)-GNE-987 (compound 4)，GNE-987 (BET 降解剂) 的羟脯氨酸差向异构体，可消除与von Hippel-Lindau的结合，不能降解BRD4蛋白。(S)-GNE-987 结合 BRD4 BD1 (IC50=4 nM) 和 BD2 (3.9 nM) 溴结构域，可用于设计PROTAC-Antibody 偶联物 (PAC)。
| 生物活性 | (S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding tovon Hippel-Lindauand does not degradeBRD4protein. (S)-GNE-987 binds to theBRD4BD1(IC50=4 nM) andBD2(3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC)[1]. |
| IC50& Target[1] | BRD4 (BD1) 4 nM (IC50) | BRD4 (BD2) 3.9 nM (IC50) | VHL |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
