Showing 1249–1264 of 5741 results

CPI-360

CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.

CB-839

CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.

PND-1186 (VS-4718)

PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1.

OTS514 Hydrochloride

OTS514 is a highly potent TOPK(T-LAK cell-originated protein kinase) inhibitor with an IC50 value of 2.6 nM.

SB225002

SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

MI-773 (SAR405838)

MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

Voxtalisib (XL765, SAR245409)

Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM also inhibits DNA-PK and mTOR. Phase 1/2.

Pilaralisib (XL147)

Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.

PF-431396

PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.

D 4476

D 4476 is a potent, selective, and cell-permeant CK1 (casein kinase 1) inhibitor with IC50 of 200 nM and 300 nM in a cell-free assay for CK1 from Schizosaccharomyces pombe and CK1δ, respectively. Also acts as an ALK5 inhibitor with IC50 of 500 nM.

Remodelin

Remodelin is a potent acetyl-transferase NAT10 inhibitor.

3PO

3PO is a small-molecule inhibitor of PFKFB3 with an IC50 of 22.9 μM for recombinant human PFKFB3 protein and does not inhibit PFK-1 activity. It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.

LDC1267

LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.

DTP3

DTP3 is a selective GADD45β/MKK7 inhibitor, which inhibits cancer-selective NF-κB survival pathway.