FPH1 (also known as BRD-6125) is a small molecule that promotes expansion of iPS-derived hepatocytes. FPH1 belongs to the functional proliferation hits which are screened out by their ability to permit renewable sourcing of functional human hepatocytes. This ability of FPH1 is not dependent on the donors of the hepatocytes. It has been found that […]
AI-10-49 is a potent and selective inhibitor of the binding of CBFβ-SMMHC to RUNX1 with IC50 of 260 nM. AI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics, and delays leukemia progression in mice. Treatment of primary inv(16) AML patient with AI-10-49 triggers selective cell death. Direct inhibition of the oncogenic CBFβ-SMMHC fusion protein may be […]
Linaprazan (also known as AZD0865) is a novel, potent inhibitor of gastric H(+),K(+)-ATPase that inhibit acid formation in vitro with a fast onset of effect. AZD0865 belongs to a new class of acid-suppressing agents with rapid onset of action and potent acid inhibition. It inhibits gastric H(+),K(+)-ATPase by K(+)-competitive binding. In porcine ion-leaky vesicles at […]
OATD-01 is a novel, selective and highly active CHIT1 (chitinase1, hAMCase IC50=9nM, hCHIT1 IC50=26nM) inhibitor with both an excellent PK profile in multiple species and selectivity against a panel of other off-targets.
GSK484 is a novel, potent, selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor which showes high affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium.
SGX-523 (SGX 523; SGX523) is a novel, exquisitely selective, and ATP-competitive inhibitor of Hepatocyte growth factor receptor/Met with potential anticancer activity.
TRC051384 is a novel compound which can potently induce HSPA1A/B (heat shock protein) expression and subsequent Hsp70 production via heat shock factor-1 (HSF1) activation.