A Bcl-xL inhibitor
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WEHI-539 (hydrochloride)

Item No. 44330

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[3-[4-(aminomethyl)phenoxy]propyl]-2-[8-[2-(2-benzothiazolyl)hydrazinylidene]-5,6,7,8-tetrahydro-2-naphthalenyl]-4-thiazolecarboxylic acid, monohydrochloride
CAS Number
2070018-33-4
Molecular Formula
C31H29N5O3S2 • HCl
Formula Weight
620.2
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/mlWater: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(C1=C(CCCOC2=CC=C(CN)C=C2)SC(C3=CC(C(CCC4)=NNC5=NC6=C(S5)C=CC=C6)=C4C=C3)=N1)O.Cl
InChi Code
InChI=1S/C31H29N5O3S2.ClH/c32-18-19-10-14-22(15-11-19)39-16-4-9-27-28(30(37)38)34-29(40-27)21-13-12-20-5-3-7-24(23(20)17-21)35-36-31-33-25-6-1-2-8-26(25)41-31;/h1-2,6,8,10-15,17H,3-5,7,9,16,18,32H2,(H,33,36)(H,37,38);1H
InChi Key
GJBYTVIQTMIXGA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $63

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    5 mg

    $257

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    10 mg

    $454

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    Cayman Chemical
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    Product Description

    WEHI-539 is an inhibitor of Bcl-xL (IC50 = 1.1 nM).1 It selectively binds to Bcl-xL (Kd = 1.4 nM) over Bcl-2, myeloid cell leukemia-1 (Mcl-1), Bcl-W, and Bfl-1, also known as Bcl-2-related protein A1 (Kds = >750, >550, >550, and >550 nM, respectively). It selectively induces apoptosis in Mcl-1-deficient mouse embryonic fibroblasts (MEFs) over wild-type MEFs, Bcl-xL- or Bcl-2-deficient MEFs, and Mcl-1-overexpressing MEFs. WEHI-539 (1 µM) also induces apoptosis in SW480 colorectal cancer cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lessene, G., Czabotar, P.E., Sleebs, B.E., et al. Structure-guided design of a selective BCL-XL inhibitor. ACS Med. Chem. Lett. 5(6), 662-667 (2014).

    2. Scherr, A.L., Mock, A., Gdynia, G., et al. Identification of BCL-XL as highly active survival factor and promising therapeutic target in colorectal cancer. Cell Death Dis. 11(10), 875 (2020).