A potent inhibitor of LDHA and LDHB
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GSK2837808A

Item No. 20626

Technical Information
Formal Name
3-[[3-[(cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)-benzoic acid
CAS Number
1445879-21-9
Molecular Formula
C31H25F2N5O7S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: slightly soluble
λmax
223, 266 nm
SMILES
FC1=CC(F)=CC(OC2=CC(C(O)=O)=CC(NC3=C(S(NC4CC4)(=O)=O)C=NC5=C3C=CC(C6=C(OC)N=C(OC)N=C6)=C5)=C2)=C1
InChi Code
InChI=1S/C31H25F2N5O7S/c1-43-29-25(14-35-31(37-29)44-2)16-3-6-24-26(9-16)34-15-27(46(41,42)38-20-4-5-20)28(24)36-21-7-17(30(39)40)8-22(13-21)45-23-11-18(32)10-19(33)12-23/h3,6-15,20,38H,4-5H2,1-2H3,(H,34,36)(H,39,40)
InChi Key
RZBCPMYJIARMGV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GSK2837808A is a potent inhibitor of lactate dehydrogenase (LDH) A and B (IC50s = 2.6 and 0.43 nM, for human recombinant LDHA and LDHB, respectively).1 It inhibits lactate production in Snu398 hepatocellular carcinoma cells in which LDHB expression is undetectable (EC50 = 400 nM). GSK2837808A (10 µM) reduces glucose consumption in Snu398 but not HepG2 hepatocellular carcinoma cells. A panel of 30 cancer cell lines, with varying levels of LDHA and LDHB expression, shows differential sensitivities to GSK2837808A with EC50s ranging from 400 nM to 30 µM. The potency of GSK2837808A does not correlate with LDHA, LDHB, or total LDH expression levels.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Billiard, J., Dennison, J.B., Briand, J., et alQuinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 1(1), 19 (2013).