Description WEHI-539 HCl (WEHI-539 hydrochloride) has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. It has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members. In vitro WEHI-539 shows good selectivity for BCL-XL. The tight ligand WEHI-539 retains this selectivity (500-fold over BCL-2 and 400-fold over BCL-W, MCL-1 and A1). WEHI-539 kills fibroblasts that lack MCL-1. Thus, WEHI-539 not only binds very tightly to BCL-XL, with IC50 and KD values close to or below 1 nM as well as a slow dissociation rate, but also invokes apoptotic responses that depend on BAX, BAK or both; furthermore, its biological activity is related to its binding profile, as elevated amounts of MCL-1, BCL-2 and BCL-W confer marked resistance, and its ability to destroy platelets is a well-validated marker of on-target BCL-XL inhibition. In addition, WEHI-539 induces a preferentially BAK-dependent apoptotic response in MEFs by selectively inhibiting BCL-XL
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WEHI-539 HCl
CAS number：2070018-33-4 molecular formula：C31H29N5O3S2.HCl
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| Chinese alias | WEHI-539 盐酸 | ||
| English alias | WEHI-539 hydrochloride | ||
| CAS number | 2070018-33-4 | molecular formula | C31H29N5O3S2.HCl |
| molecular weight | 620.18 g/mol | Exact mass | ≥97% |
| PSA | - | logp | - |
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