A PKCθ inhibitor
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VTX-27

Item No. 36938

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αR,2S)-4-[3-chloro-5-fluoro-6-(1H-pyrazolo[3,4-b]pyridin-3-yl)-2-pyridinyl]-α-methyl-α-(1-methylethyl)-2-piperazinemethanol
CAS Number
1321924-70-2
Molecular Formula
C20H24ClFN6O
Formula Weight
418.9
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
FC1=C(N=C(N2C[C@@](NCC2)([H])[C@](C)(O)C(C)C)C(Cl)=C1)C3=NNC4=NC=CC=C34
InChi Code
InChI=1S/C20H24ClFN6O/c1-11(2)20(3,29)15-10-28(8-7-23-15)19-13(21)9-14(22)17(25-19)16-12-5-4-6-24-18(12)27-26-16/h4-6,9,11,15,23,29H,7-8,10H2,1-3H3,(H,24,26,27)/t15-,20+/m0/s1
InChi Key
HXWARSZQGAFXJM-MGPUTAFESA-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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    500 µg

    $106

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    1 mg

    $202

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    Product Description

    VTX-27 is a PKCθ inhibitor (Ki = 0.08 nM).1 It is selective for PKCθ over PKCα, -βI, -βII, -γ, -δ, -ε, -η, -µ, and -ζ with Ki values ranging from 1 to >5,000 nM as well as a panel of seven kinases from the Src, spleen tyrosine kinase (Syk), Tec, and MAP kinase families (Kis = >1,000 nM for all). VTX-27 inhibits CD28-induced IL-2 release in isolated human peripheral blood mononuclear cells (PBMCs; IC50 = 11 nM). Oral administration of VTX-27 (12.5, 25, and 50 mg/kg) prevents staphylococcal enterotoxin B-induced increases in IL-2 plasma levels in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jimenez, J.-M., Boyall, D., Brenchley, G., et al. Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases. J. Med. Chem. 56(5), 1799-1810 (2013).