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LDHA 5W8J 3d printed

DIGITAL PREVIEW
Not a Photo

Glossy Full Color Sandstone
LDHA 5W8J 3d printed
LDHA 5W8J 3d printed

DIGITAL PREVIEW
Not a Photo

LDHA 5W8J

Made by
$255.96
3D printed in fully colored material with a glossy and smooth finish.
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Product Description
We report the discovery and medicinal chemistry optimization of a novel series of pyrazole-based inhibitors of human lactate dehydrogenase (LDH). Utilization of a quantitative high-throughput screening paradigm facilitated hit identification, while structure-based design and multiparameter optimization enabled the development of compounds with potent enzymatic and cell-based inhibition of LDH enzymatic activity. Lead compounds such as 63 exhibit low nM inhibition of both LDHA and LDHB, submicromolar inhibition of lactate production, and inhibition of glycolysis in MiaPaCa2 pancreatic cancer and A673 sarcoma cells. Moreover, robust target engagement of LDHA by lead compounds was demonstrated using the cellular thermal shift assay (CETSA), and drug-target residence time was determined via SPR. Analysis of these data suggests that drug-target residence time (off-rate) may be an important attribute to consider for obtaining potent cell-based inhibition of this cancer metabolism target
Details
What's in the box:
mdm_LDHA_5W8J_max_v17
Dimensions:
11.91 x 6.43 x 7.76 cm
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4.69 x 2.53 x 3.05 inches
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Success Rate:
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Rating:
Mature audiences only.
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