Chemical Structure : HPK1 PROTAC SS44
货号: PC-72307Not For Human Use, Lab Use Only.
HPK1 PROTAC SS44 is a heterobifunctional small molecule HPK1 PROTAC degrader based on ZYF0033 that simultaneously binds HPK1 and E3 ligase Cereblon (CRBN), induces degradation of HPK1.
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HPK1 PROTAC SS44 is a heterobifunctional small molecule HPK1 PROTAC degrader based on ZYF0033 that simultaneously binds HPK1 and E3 ligase Cereblon (CRBN), induces degradation of HPK1.
SS44 (100 nM) caused significant degradation of HPK1 within 12 h after SS44 treatment in human PBMCs withno significant IKZF1/3 degradation, which could be blocked by treatment with the proteasome inhibitor MG132 and with the NEDD8-activating enzyme (NAE) inhibitor MLN4924.
SS44 showed markedly stronger inhibition of tumor growth, significantly enhanced the antitumor efficacy of anti-PD-1 antibody treatment.
分子量 | 875.054 | |
分子式 | C48H54N6O8S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Jingwen Si, et al. Cancer Cell. 2020 Oct 12;38(4):551-566.e11.
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