An inhibitor of VprBP
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B32B3

Item No. 16364

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)hydrazone 1H-indole-3-carboxaldehyde
CAS Number
294193-86-5
Synonyms
  • VprBP Inhibitor
Molecular Formula
C19H17N5S
Formula Weight
347.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 15 mg/ml
λmax
225, 269, 345 nm
SMILES
C1(C(N/N=C/C2=CNC3=C2C=CC=C3)=NC=N4)=C4SC5=C1CCCC5
InChi Code
InChI=1S/C19H17N5S/c1-3-7-15-13(5-1)12(9-20-15)10-23-24-18-17-14-6-2-4-8-16(14)25-19(17)22-11-21-18/h1,3,5,7,9-11,20H,2,4,6,8H2,(H,21,22,24)/b23-10+
InChi Key
AKDKHZVFMAWBFX-AUEPDCJTSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $64

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    10 mg

    $121

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    25 mg

    $288

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    Cayman Chemical
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    Product Description

    B32B3 is a cell-permeable, ATP-competitive inhibitor of VprBP that blocks phosphorylation of histone 2A at Thr120 in DU-145 human prostate cancer cells (IC50 = 500 nM).1 It exhibits over 100-fold selectivity for VprBP against a panel of 33 other protein kinases.1 B32B3 strongly suppresses the proliferation of DU-145 cells, which overexpress VprBP, but not MCL normal human prostate cells, which have low levels of VprBP expression.1 At 5 mg/kg twice a week over three weeks, B32B3 inhibits the growth of DU-145 xenograft tumors in mice by 70-75%.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kim, K., Kim, J.M., Kim, J.S., et al. VprBP has intrinsic kinase activity targeting histone H2A and represses gene transcription. Mol. Cell 52(3), 459-467 (2013).