An LDHA and LDHB inhibitor
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LDH-IN-1

Item No. 44281

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[4-[[4-(aminosulfonyl)phenyl]methyl]-3-[1,1′-biphenyl]-3-yl-5-(cyclopropylmethyl)-1H-pyrazol-1-yl]-4-thiazolecarboxylic acid
CAS Number
1964515-43-2
Synonyms
  • Lactate Dehydrogenase-IN-1
  • Lactate Dehydrogenase Inhibitor 1
  • LDH Inhibitor 1
Molecular Formula
C30H26N4O4S2
Formula Weight
570.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
NS(C(C=C1)=CC=C1CC(C(C2=CC(C3=CC=CC=C3)=CC=C2)=NN4C5=NC(C(O)=O)=CS5)=C4CC6CC6)(=O)=O
InChi Code
InChI=1S/C30H26N4O4S2/c31-40(37,38)24-13-11-19(12-14-24)15-25-27(16-20-9-10-20)34(30-32-26(18-39-30)29(35)36)33-28(25)23-8-4-7-22(17-23)21-5-2-1-3-6-21/h1-8,11-14,17-18,20H,9-10,15-16H2,(H,35,36)(H2,31,37,38)
InChi Key
ALJORCZKMBZYCR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $83

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    5 mg

    $351

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    10 mg

    $537

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    25 mg

    $825

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    Product Description

    LDH-IN-1 is an inhibitor of lactate dehydrogenase A (LDHA) and LDHB (IC50s = 0.032 and 0.027 µM, respectively).1 It is selective for LDHA and LDHB over malate dehydrogenase (MDH) and isocitrate dehydrogenase 1 (IDH1; IC50s = 37.8 and 29.8 µM, respectively). LDH-IN-1 is cytotoxic to A-673 sarcoma and MiaPaCa-2 pancreatic cancer cells (IC50s = 2.9 and 3.96 µM, respectively). It decreases the extracellular acidification rate (ECAR) in A-673 cells when used at concentrations ranging from 2 to 10 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rai, G., Brimacombe, K.R., Mott, B.T., et al. Discovery and optimization of potent, cell-active pyrazole-based inhibitors of lactate dehydrogenase (LDH). J. Med. Chem. 60(22), 9184-9204 (2017).