Showing 769–784 of 5741 results

TAK-659

TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.

LW 6

LW6 is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. LW6 inhibits HIF and MDH2 expression with IC50 values of 4.4 and 6.3 μM, respectively.

B02

B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM).

NS-398 (NS398)

NS-398 is a selective inhibitor of cyclooxygenase-2 (COX-2). The IC50 values for human recombinant COX-1 and -2 are 75 and 1.77 μM, respectively.

Troglitazone (CS-045)

Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth.

LTURM34

LTURM34 is a specific DNA-PK inhibitor, 170-fold more selective for DNA-PK activity compared to PI3K activity, with IC50 value of 0.034 μM.

10074-G5

10074-G5 is a c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM).

R-IMPP

R-IMPP is an inhibitor of PCSK9 secretion, half maximal inhibitory concentration [IC50] = 4.8 μM.

E7449

E7449 is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively.

PACAP 6-38

PACAP 6-38 is a PACAP (pituitary adenylate cyclase-activating polypeptide) non-stimulating competitive antagonist with an IC50 value of 2 nM. It also acts as a functional CARTp antagonist in vivo.

PACAP 1-38

PACAP 1-38 is a highly potent PACAP receptor agonist (Kd = 100 pM). It stimulates adenylate cyclase and phagocytosis.

PACAP 1-27

Pituitary adenylate cyclase activating polypeptide (PACAP 1-27) is a potent PACAP receptor antagonist.

Naquotinib (ASP8273)

Naquotinib(ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.

PF-06273340

PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.