Chemical Structure : (R)-SL18
货号: PC-20755Not For Human Use, Lab Use Only.
(R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM.
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(R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM.
(R)-SL18 directly binds to ANXA3 (SPR Kd=0.58 uM) and increases its ubiquitination, thereby inducing ANXA3 degradation with moderate family selectivity.
(R)-SL18 inhibits cell proliferation against TNBC cells with IC50 of 2.52 uM for MDA-MB-231 and 1.64 uM for MDA-MB-468, induces apoptosis.
(R)-SL18 showed certain selectivity for the anti-proliferative activity of ANXA3 high-expressing cells over ANXA3 low-expressing cells.
(R)-SL18 induced ANXA3 selective degradation mainly via the ubiquitin-proteasome system.
(R)-SL18 showed excellent family selectivity toward ANXA3 degradation (except ANXA6) in vitro.
(R)-SL18 (1-5 uM) inhibited the wnt/β-catenin signaling pathway in MDA-MB-231 cells.
(R)-SL18 (20 mg/kg, i.p.) suppressed tumor growth in TNBC PDX model.
分子量 | 597.06 | |
分子式 | C26H21ClN6O5S2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Liang Y, et al. Acta Pharm Sin B. 2023 Apr;13(4):1686-1698.
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