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AXKO-0046

Chemical Structure : AXKO-0046

CAS No.:

AXKO-0046 (AXKO0046)

Catalog No.: PC-72514Not For Human Use, Lab Use Only.

AXKO-0046 (AXKO0046) is the first highly selective, small molecule inhibitor of human lactate dehydrogenase B (LDHB), exhibits uncompetitive LDHB inhibition with EC50 of 42 nM.

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Biological Activity

AXKO-0046 (AXKO0046) is the first highly selective, small molecule inhibitor of human lactate dehydrogenase B (LDHB), exhibits uncompetitive LDHB inhibition with EC50 of 42 nM.
AXKO-0046 selectively inhibited LDHB activity in an uncompetitive manner with respect to NADH and pyruvate, no inhibitory activity against LDHA at 300 uM.
AXKO-0046 did not bind in the catalytic site of the enzyme but significantly bound to LDHB in the novel allosteric site of the tetramer.
AXKO-0046 is a promising chemical probe to elucidate the role of LDHB-associated pathways in cancer metabolism.

Physicochemical Properties

M.Wt 375.56
Formula C25H33N3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-({3-[2-(benzylamino) ethyl]-1H-indol-2-yl} methyl) cycloheptanamine

References

1. Sachio Shibata, et al. Sci Rep. 2021 Nov 1;11(1):21353.

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