WEHI-539 hydrochloride

WEHI-539 hydrochloride

Catalog Number:
L002369647APE
Mfr. No.:
APE-A8634
Price:
$436
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      • Overview
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          Background

          WEHI-539 hydrochloride is a small-molecule inhibitor of BCL XL with IC50 value of 1.1 nM [1].
          WEHI-539 was designed as a BCL-XL inhibitor with high affinity. It interacted with the binding groove of BCL-XL with Kd value of 0.6 nM. In MEF cells lacking MCL-1, WEHI-539 induced apoptosis which was evidenced by the release of mitochondrial cytochrome c and caspase-3 processing. In BCL-XL overexpressed MEF cells, WEHI-539 showed EC50 value of 0.48 μM. WEHI-539 also significantly induced apoptosis of the platelets purified from mice. Besides that, WEHI-539 cannot kill MEF cells lacking BAK because the cell death mediator BAK is regulated by BCL-XL and MCL-1. [1].

      • Properties
        • Alternative Name
          (E)-5-(3-(4-(aminomethyl)phenoxy)propyl)-2-(8-(2-(benzo[d]thiazol-2-yl)hydrazono)-5,6,7,8-tetrahydronaphthalen-2-yl)thiazole-4-carboxylic acid
          CAS Number
          2070018-33-4
          Molecular Formula
          C31H30ClN5O3S2
          Molecular Weight
          620.18
          Appearance
          A solid
          Purity
          99.15%
          Solubility
          ≥28.55 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Kim YJ, Tsang T, et al. "Inhibition of BCL2 family members increases the efficacy of copper chelation in BRAFV600E-driven melanoma." Cancer Res. 2020;canres.1784.2019. PMID:32005716
          2. Rose JC, Dieter EM, et al. "Examining RAS pathway rewiring with a chemically inducible activator of RAS." Small GTPases. 2018 Apr 10:1-8. PMID:29634387

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