Novel TRPM8 channel blocker

CCT129202 is a potent, selective, ATP-competitive pan-Aurora kinase inhibitor with IC50 of 42, 198 and 227 nM for Aurora A, Aurora B and Aurora C, respectively.

NS-018 maleate (NS018, Ilginatinib) is a potent and highly selective JAK2 inhibitor (IC50=0.72 nM).

AZ12216052 is a mGluR II and III activator.

ML 351 is a selective 12/15 LOX inhibitor that is active in vivo.

MJ-15 is a potent and selective antagonist of cannabinoid CB1 receptor.

Arcyriaflavin A is an inhibitor of cdk4/cyclin D1 and CaM kinase II.

NSC 625987 is a potent, selective CDK4 inhibitor with IC50 of 0.2 uM, displays >500-fold selectivity over CDK2 (IC50 >100 uM for cdc2/cyclin A, cdk2/cyclin A and cdk2/cyclin E). .

VU0155069 is a potent, selective phospholipase D1 (PLD1) inhibitor with IC50 of 46 nM, 20-fold selectivity over PLD2 (IC50=933 nM).

TL02-59 is a potent, selective, orally available inhibitor of Src-family kinase Fgr IC50 of 0.03 nM, also inhibits Lyn and Hck with IC50 of 0.1 and 160 nM, respectively.

CXCR7 antagonist-1 is an inhibitor of the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR. CXCR7 antagonist-1 prevents tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128).

Chlorantraniliprole is an insecticide that potently and selectively activates insect ryanodine receptor, with EC50s of 40 nM and 50 nM for Drosophila melanogaster and H. virescens ryanodine receptor, and ∼300-fold more potent than that in the mouse myobla

NVP-MELK8a hydrochloride (MELK8a hydrochloride) is a novel potent, and selective MELK inhibitor with IC50 of 2 nM.

NMS-E973 is a novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). NMS-E973 displays significant efficacy in a human ovarian A2780 xenograft tumor model, with a mechanism of action confirmed in vivo by typical modulation of known Hsp90 client proteins, and with a favorable pharmacokinetic and safety profile. The efficacy profile of NMS-E973 suggests a potential for development in different clinical settings, including tumors that have become resistant to molecular targeted agents, particularly in cases of tumors which reside beyond the blood-brain barrier (BBB).

Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist.

CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.

Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties.

LP-935509 is a potent inhibitor of the Adapter protein-2 Associated Kinase 1 (AAK1).

For the detailed information of SR10067, the solubility of SR10067 in water, the solubility of SR10067 in DMSO, the solubility of SR10067 in PBS buffer, the animal experiment (test) of SR10067, the cell expriment (test) of SR10067, the in vivo, in vitro and clinical trial test of SR10067, the EC50, IC50,and affinity,of SR10067, For the detailed information of SR10067, the solubility of SR10067 in water, the solubility of SR10067 in DMSO, the solubility of SR10067 in PBS buffer, the animal experiment (test) of SR10067, the cell expriment (test) of SR10067, the in vivo, in vitro and clinical trial test of SR10067, the EC50, IC50,and affinity,of SR10067, Please contact DC Chemicals..

NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.

LSN2463359 is a novel positive allosteric modulators of the mGlu? receptor.

A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM.

Ulixertinib, also known as BVD-523 and VRT752271, is an inhibitors of ERK protein kinase. Downmodulation of ERK protein kinase activity inhibits VEGF secretion by human myeloma cells and myeloma-induced angiogenesis. Upon oral administration, BVD-523 inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.

DY-268 is a trisubstituted-pyrazol carboamide based compound that acts as a potent FXR antagonist (IC50 = 7.5 nM). It does not display any FXR agonistic activity and cytotoxicity.

GSK854 is a potent Inhibitor of Troponin I-Interacting Kinase (TNNI3K). GSK854 is a suitable lead for identifying new cardiac medicines and have been employed as in vivo tools in investigational studies aimed at defining the role of TNNI3K within heart failure.

A potent, selective, and centrally active positive allosteric modulator of AMPAR-mediated neurotransmission, which increase ion channel flux in the presence of agonist by suppressing desensitization and/or deactivation of the receptors..

A novel potent, selective and orally active enterocytic microsomal triglyceride transfer protein (MTP) inhibitor that inhibits only MTP localized to enterocytes with IC50 of 6 nM.

CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties.

BAY-1797 is a potent and selective P2X4 antagonist.

K-756 is a a selective Wnt/β-catenin pathway inhibitor. K-756 is also a tankyrase (TNKS) inhibitor. K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. could be a leading compound in the development of anticancer agents.