A GSK3α inhibitor
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BRD0705

Item No. 37314

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(4S)-4-ethyl-1,2,4,6,7,8-hexahydro-7,7-dimethyl-4-phenyl-5H-pyrazolo[3,4-b]quinolin-5-one
CAS Number
2056261-41-5
Molecular Formula
C20H23N3O
Formula Weight
321.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: solubleMethanol: soluble
λmax
331 nm
SMILES
CC(C)(CC1=O)CC2=C1[C@](C3=CC=CC=C3)(CC)C4=CNN=C4N2
InChi Code
InChI=1S/C20H23N3O/c1-4-20(13-8-6-5-7-9-13)14-12-21-23-18(14)22-15-10-19(2,3)11-16(24)17(15)20/h5-9,12H,4,10-11H2,1-3H3,(H2,21,22,23)/t20-/m0/s1
InChi Key
NCKLQXXBRWCYMA-FQEVSTJZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    BRD0705 is an inhibitor of glycogen synthase kinase 3α (GSK3α; IC50 = 66 nM).1 It is selective for GSK3α over GSK3β (IC50 = 515 nM). BRD0705 (10 and 20 µM) inhibits GSK3α autophosphorylation in U937 cells. It impairs colony formation of MOLM-13, TF-1, U937, MV4-11, HL-60, and NB4 acute myeloid leukemia (AML) cells. In vivo, BRD0705 (30 mg/kg) inhibits leukemia development in secondary recipient mice in an MLL-AF9 mouse syngeneic tumor model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wagner, F.F., Benajiba, L., Campbell, A.J., et al. Exploiting an Asp-Glu "switch" in glycogen synthase kinase 3 to design paralog-selective inhibitors for use in acute myeloid leukemia. Sci. Transl. Med. 10(431), eaam8460 (2018).