A BET BD2 inhibitor
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GSK620

Item No. 36139

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N5-cyclopropyl-1,2-dihydro-N3-methyl-2-oxo-1-(phenylmethyl)-3,5-pyridinedicarboxamide
CAS Number
2088410-46-0
Molecular Formula
C18H19N3O3
Formula Weight
325.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/ml
SMILES
O=C(C(C=C1C(NC)=O)=CN(CC2=CC=CC=C2)C1=O)NC3CC3
InChi Code
InChI=1S/C18H19N3O3/c1-19-17(23)15-9-13(16(22)20-14-7-8-14)11-21(18(15)24)10-12-5-3-2-4-6-12/h2-6,9,11,14H,7-8,10H2,1H3,(H,19,23)(H,20,22)
InChi Key
QZZCUOVXHPAQRQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $61

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    10 mg

    $116

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    25 mg

    $242

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    50 mg

    $455

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    Product Description

    GSK620 is a bromodomain and extra terminal domain family of proteins (BET) bromodomain 2 (BD2) inhibitor (IC50s = 316.2, 79.4, 79.4, and 199.5 nM for BRD2, BRD3, BRD4, and BRDT BD2, respectively).1 It is selective for BD2 in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and BRDT over BD1 in the same BRDs (IC50s = >15,000 nM for all). GSK620 inhibits LPS-induced chemokine (C-C motif) ligand 1 (CCL1) production in isolated human whole blood (IC50 = 794.3 nM). See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Seal, J.T., Atkinson, S.J., Aylott, H., et al. The optimization of a novel, weak bromo and extra terminal domain (BET) bromodomain fragment ligand to a potent and selective second bromodomain (BD2) inhibitor. J. Med. Chem. 63(17), 9093-9126 (2020).