Showing 1569–1584 of 7558 results

BMS-345541

BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively.

Scriptaid

Scriptaid is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.

GW2580

GW2580 is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.

Cobimetinib (GDC-0973, RG7420)

Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Phase 3.

GDC-0349

GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.

PU-H71

PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.

UPF 1069

UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.

Necrostatin-1

Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells.

Butein

Butein, a plant polyphenol isolated from Rhus verniciflua, is able to inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, also inhibits EGFR.

VU 0364439

VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.

PRT062607 (P505-15, BIIB057) HCl

PRT062607 (P505-15, BIIB057) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.

NSC 23766

NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay does not inhibit the closely related targets, Cdc42 or RhoA.

Plerixafor (AMD3100)

Plerixafor (AMD3100) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively.

WY-14643 (Pirinixic Acid)

WY 14643 (Pirinixic Acid) is a potent peroxisome proliferator and activator of PPARα with EC50 of 1.5 μM.

Tariquidar

Tariquidar is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM in CHrB30 cell line, reverses drug resistance in MDR cell Lines. Phase 3.

GSK3787

GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.