CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM. CADD522 treatment resulted in significant growth inhibition, clonogenic survival, tumorsphere formation, and invasion of breast cancer cells. CADD522 negatively regulated transcription of RUNX2 target genes such as matrix metalloproteinase-13, vascular endothelial growth factor and glucose transporter-1, but upregulated RUNX2 expression by increasing RUNX2 stability. CADD522 reduced RUNX2-mediated increases in glucose uptake and decreased the level of CBF-β and RUNX2 phosphorylation at the S451 residue.

Torezolid (TR-701; tedizolid) is a novel oxazolidinone for gram-positive infections.

Motesanib is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.

Splitomicin is a derivative of β-naphthol is an inhibitor of Silent Information Regulator 2 (SIR2).

CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM, shows cytotoxicity against a broad CLL samples with mean LD50 of 80 nM.

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.

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

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.

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

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.

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