A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.

Baloxavir acid (S-033447) is an anti-influenza compound that potently and selectively inhibits the cap-dependent endonuclease within the polymerase PA subunit of influenza A and B viruses.

(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.

Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1].

S29434 (S 29434) is a highly potent, selective, cell-active inhibitor of Quinone reductase 2 (QR2) with IC50 of 5-16 nM, shows good selectivity for QR2 over QR1.

LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects.

FTBMT is a novel selective GPR52 agonist of GPR52, increases intracellular cAMP levels in CHO cells expressing human, mouse, or rat GPR52, with pEC50 of 7.03, 6.85, and 6.87M, respectively.

N-Succinimidyl S-acetylthioacetate (SATA), a protein modification agent, introduces thiol-groups into protein molecules. N-Succinimidyl S-acetylthioacetate adds sulfhydryl groups to proteins and other amine-containing molecules in a protected form.

S119-8 is a novel broad spectrum inhibitor of influenza virus replication (IC50=1.43 nM) by targeting the viral Nucleoprotein (NP), with no detectable cytotoxicity (CC50>50 uM).

MCP110 is a potent Ras/Raf-1 interaction inhibitor.

TCN-201 is a selective antagonist of NMDA receptors containing the NR2A subunit. TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner.

JWG-071 is the first reported kinase-selective chemical probe for ERK5. JWG-071 improves ERK5 activity and BRD4 selectivity. JWG-071 will be a much-needed chemical probe for deconvoluting ERK5 and BRD4 pharmacology[1].

GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells)[1].

GW 6471 is a potent PPARα antagonist.

ABT-869 is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of the vascular endothelial growth factor (VEGF) and platelet derived growth factor (PDGF) receptor families.

AP24534 is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.

AMG-Tie2-1 is a highly potent, non-selective inhibitor of Tie-2 (IC50 <1 nM).

AZD-26 is an inhibitor of AKT. AZD-26 inhibits the phosphorylation of Thr308 on AKT in BT474 cells with an IC50 of 422 nM.

AZ9482, a potent and selective PARP inhibitor featuring an amide linkage to a 2-piperazinyl-3-cyano-pyridine.

AZD8330(ARRY-424704; ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM.

Bayer-18 is a selective TYK2 inhibitor, with an IC50 of 18.7nM on TYK2 as measured by TYK2 HTRF assays.

BGG463 can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 μM, 0.09 μM and 0.590 μM, respectively.

BIX 02565 is a novel ribosomal S6 kinase 2 (RSK2) inhibitor with an IC50 of 1.1 nM.

CFI-400437 is potent against PLK4 (IC50 = 0.6 nM) and selective against other members of the PLK family (>10 uM).

Canertinib (CI-1033) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3. CI-1033 shows excellent potency for irreversible inhibition of erbB2 autophosphorylation in MDA-MB

Dianilinopyrimidine_01 is a Pan Tyrosine kinase inhibitor.

LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.

Mubritinib is a potent inhibitor of the human epidermal growth factor receptor 2 (HER2) tyrosine kinase.

PD-173955 is a src tyrosine kinase inhibitor. PD173955 inhibited Bcr-Abl-dependent cell growth.

SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po).