LDN-193189 | BMP type I receptors ALK2/3 inhibitorCellagen TechnologyPrice from $109.00 to $981.00.
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Cellagen Technology
BRD2/3/4 inhibitor
GSK1210151A (I-BET151) is an orally-available, imidazolonoquinoline-based inhibitor of the BET family of bromodomains, active against BRD2, BRD3, and BRD4 at IC50s of 500, 250, and 800 nM, respectively. It is also a potent upregulator of ApoA1 with an EC170 of 100 nM. [1]
GSK1210151A was shown to have profoudn efficacy against human and murine MLL-fusion leukemic cell lines, through the induction of early cell cycle arrest and apoptosis. The mode of action is partly due to the inhibition of transcrdiption of key genes (BCL2, C-MYC, and CDK6) through the displacement of BRD3/4, PAFc, and SEC components through chromatin. [2]
Because ApoA1 upregulation is often associated with anti-inflammatory properties in non hepatic cells, GSK1210151A was tested and shown to exhibit a dose-dependent inhibition of both IL-6 and TNFa production in LPS-stimulated human PBMCs. [3]
Cellagen Technology
BRD2/3/4 inhibitor
GSK1210151A (I-BET151) is an orally-available, imidazolonoquinoline-based inhibitor of the BET family of bromodomains, active against BRD2, BRD3, and BRD4 at IC50s of 500, 250, and 800 nM, respectively. It is also a potent upregulator of ApoA1 with an EC170 of 100 nM. [1]
GSK1210151A was shown to have profoudn efficacy against human and murine MLL-fusion leukemic cell lines, through the induction of early cell cycle arrest and apoptosis. The mode of action is partly due to the inhibition of transcrdiption of key genes (BCL2, C-MYC, and CDK6) through the displacement of BRD3/4, PAFc, and SEC components through chromatin. [2]
Because ApoA1 upregulation is often associated with anti-inflammatory properties in non hepatic cells, GSK1210151A was tested and shown to exhibit a dose-dependent inhibition of both IL-6 and TNFa production in LPS-stimulated human PBMCs. [3]
