A DGK-α inhibitor
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BMS 684

Item No. 46736

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-(diphenylmethyl)-1-piperazinyl]-1-methyl-3-2(1H)-quinolinone
CAS Number
313552-29-3
Molecular Formula
C27H26N4O3
Formula Weight
454.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CN(C1=C(C(N2CCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4)=C5[N+]([O-])=O)C=CC=C1)C5=O
InChi Code
InChI=1S/C27H26N4O3/c1-28-23-15-9-8-14-22(23)25(26(27(28)32)31(33)34)30-18-16-29(17-19-30)24(20-10-4-2-5-11-20)21-12-6-3-7-13-21/h2-15,24H,16-19H2,1H3
InChi Key
XIVOLEKHEMYRBO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $65

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    5 mg

    $293

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    10 mg

    $553

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    25 mg

    $813

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    Product Description

    BMS 684 is an inhibitor of diacylglycerol kinase α (DGK-α; IC50 = 0.0046 µM).1 It is selective for DGK-α over DGK-β, -γ, -κ, and -ζ (IC50s = 2.5, 1.9, >10, and >10 µM, respectively), a panel of 327 other kinases at 15 µM, and a panel of 42 receptors, ion channels, and enzymes at 30 µM. BMS 684 induces translocation of DGK-α to the plasma membrane in Jurkat cells (EC50 = 0.52 µM) and increases T cell receptor-mediated IL-2 levels in programmed cell death protein 1-positive (PD-1+) and PD-1- primary human CD4+ T cells.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chupak, L., Wichroski, M., Zheng, X., et al. Discovery of potent, dual-inhibitors of diacylglycerol kinases alpha and zeta guided by phenotypic optimization. ACS Med. Chem. Lett. 14(7), 929-935 (2023).

    2. Wichroski, M., Benci, J., Liu, S.Q., et al. DGKα/ζ inhibitors combine with PD-1 checkpoint therapy to promote T cell-mediated antitumor immunity. Sci. Transl. Med. 15(719), (2023).