Novel inhibitors

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Cat. No.	Product Name	Field of Application
DC23117	GV-58	GV-58 is a potent, selective N-Type and P/Q-type Ca2+ Channel agonist with EC50 of 7.2 and 8.8 uM, shows no acitivity for L-type calcium channels (EC50>100 uM).
DC9458	GW-1100	GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120, another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99.
DC21102	GW 275175X	GW 275175X is a derivative of BDCRB that displays anti-HCMV activity by inhibition of viral DNA maturation.
DC23402	GW 841819X	GW 841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomain that displays activity in vivo against NUT-midline carcinoma, multiple myeloma, mixed-lineage leukemia, and acute myeloid leukemia..
DC7149	GW1929 Featured	GW1929 is a synthetic peroxisome proliferator-activated receptor-γ (PPARγ) agonist with IC50 of 6.2 nM and 13 nM for human and mouse, respectively.
DC23142	GW274150 Featured	GW274150 is a novel arginine-competitive, NADPH-dependent iNOS inhibitor that has been identified from a series of acetamide amino acids that have a high selectivity for iNOS vs both eNOS (> 260-fold) and nNOS (> 219-fold) and high bioavailability (> 90%) after oral administration.Target: iNOSin vivo: GW274150 demonstrates a narrow neuroprotective therapeutic window against the toxic actions of 6-OHDA. GW274150 administration leads to a dose-dependent decrease in the number of iNOS-positive cells in the SNc of the 6-OHDA-lesioned animals. The iNOS inhibitor GW274150 fails to produce long-term neuroprotection after its withdrawal in the 6-OHDA-lesioned rat. [1]
DC8193	GW311616A	GW311616A is a potent, intracellular human neutrophil elastase (HNE, α-1-proteinase) inhibitor.
DC12644	GW406108X	GW406108X (GW-406108X, GW108X) is specific inhibitor of Kif15 (Kinesin-12) with IC50 of 0.82 uM in ATPase assays.
DC7980	GW-6604 Featured	GW6604 is a potent and selective ALK-5 inhibitor with potent anticancer activity.
DC23530	GW-766994 R-form	GW-766994 (GW766994) is a potent, selective, orally available CCR3 antagonist with pKi of 7.86 for inhibiting eotaxin-induced eosinophil chemotaxis in vitro assays.
DC23531	GW-766994	GW-766994 (GW766994) is a potent, selective, orally available CCR3 antagonist with pKi of 7.86 for inhibiting eotaxin-induced eosinophil chemotaxis in vitro assays.
DC22653	GW-8510 Featured	GW-8510 (GW8510) is a potent, selective inhibitor of CDK2 with IC50 of 10 nM.
DC11993	GWJ-A-23	GWJ-A-23 (GWJ-23, GWJ23) is a potent, selective autotaxin inhibitor with Ki of 18 nM, an analog of the known ATX inhibitor S32826 and has improved aqueous solubility compared with the parent compound.
DC23613	GX-936	GX-936 (PF 05196233) is a potent Nav1.7 inhibitor that binds to the activated state of voltage-sensor domain IV (VSD4), exhibits robust inhibition of the 1KαPMTX-evoked N1742K response with IC50 of 40 nM.
DC5061	GYKI 52466 dihydrochloride	GYKI 52466 dihydrochloride is a selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively). Skeletal muscle relaxant and orally-active anticonvulsant.
DC22106	GZ389988	GZ389988 (GZ-389988) is a novel potent, selective, locally delivered TrkA inhibitor for the treatment osteoarthritis.
DC20118	GZD856 Featured	GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities. Also a Bcr-AblT315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant.
DC11010	H3B-5942	H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo.
DC21105	H3B-8800 Featured	H3B8800 is an orally available splicing modulator that targets spliceosome SF3b complex containing either WT or mutant SF3B1 (binding IC50 of 0.3-2 nM),demonstrates dose-dependent inhibition of both canonical splicing and aberrant splicing induced by mutant SF3B1 in in vitro assays of biochemical splicing, induces lethality in spliceosome-mutant cancer cells.. H3B-8800 potently and preferentially kills spliceosome-mutant epithelial and hematologic tumor cells.
DC12266	H4 Receptor antagonist 1	H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.
DC20106	H4R antagonist 1	H4R antagonist 1
DC1066	HA14-1 Featured	HA14-1 is a nonpeptidic ligand of a Bcl-2 surface pocket with IC50 of~9 μM.
DC9567	Halcinonide	Halcinonide is a high potency corticosteroid used topically in the treatment of certain skin conditions.
DC9749	Halofuginone	Halofuginone is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.
DC10935	HAMI3379	HAMI3379 (HAMI-3379) is a potent and selective antagonist of cysteinyl leukotriene 2 (CysLT(2)) receptor, inhibits LTD4- and LTC4-induced intracellular calcium mobilization withIC50 of 3.8 nM and 4.4 nM respectively.
DC21106	HAP-12	HAP-12 is a small molecule HBV capsid assembly effector that inhibits HBV DNA replication with EC50 of 0.5 uM..
DC23253	HAR-171	HAR-171 is a small molecule gp120-CD40 blocker that acts as a highly potent HIV entry inhibitor with IC50 of 0.43 uM against YTA48P virus with no significant cytotoxicity (CC50>120 uM)..
DC12224	H-Arg-4MβNA	H-Arg-4MβNA is a substrate for cathepsin H, used for the detection of enzyme activity in gel electrophoresis.
DC23634	HBT1	HBT1 is a novel potent AMPA receptor potentiator with lower agonistic effect compared with LY451395 and OXP1..
DC20917	HBV Capsid inhibitor 3711	HBV Capsid inhibitor 3711 (Compound 3711) is a nonnucleosidic HBV inhibitor, inhibits hepatitis B virus replication by inducing genome-free capsid formation.

Novel inhibitors

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