Inhibitors & Agonists

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Cat. No.	Product Name	Field of Application
DC12629	CM-675	CM-675 (CM675) is a potent, dual PDE5 and classI-HDAC inhibitor with IC50 of 114/673 nM for PDE5A/HDAC1, respectively.
DC20913	CMA-008	CMA-008 is a cell-permeable, small molecule modulator of NAADP-mediated Ca2+ release, competes with NAADP binding, inhibit Ca2+ release via the NAADP receptor (IC50=15 uM-1 mM).
DCAPI1542	CMC·HCI	CMC·HCI
DC23813	CMC2.24	CMC2.24 (TRB-N0224) is a novel tricarbonylmethane agent that inhibits the Ras-RAF-MEK-ERK pathway, inhibits Ras activation in pancreatic cancer both in vitro and in vivo.
DC7388	c-Met inhibitor 1	c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.
DC9617	CMK	CMK is a RSK2 kinase inhibitor.
DC21530	CMP-5 Featured	CMP-5 (PRMT5-IN-5)is a first-in-class, small-molecule PRMT5-specific inhibitor that blocks EBV-driven B-lymphocyte transformation and survival, without effect on normal B cells.
DC21531	CMP-5 hydrochloride	CMP-5 (PRMT5-IN-5)is a first-in-class, small-molecule PRMT5-specific inhibitor that blocks EBV-driven B-lymphocyte transformation and survival, without effect on normal B cells.
DC9803	CMP8 Featured	CMP8 is a high-affinity ligand that binds only to mutant ERLBD.
DC23508	CMPD167	CMPD167 (MRK-1) is an orally acitve small molecule that binds to CCR5 to inhibit gp120 association, inhibits different stages of the virus-cell attachment and entry process (CCR5-using virus SHIV-162P3, IC50<1 nM)..
DC22512	CMPDA Featured	CMPDA is a potent positive allosteric modulator of GluR2 receptors with EC50 of 45.4 and 63.4 nM at GluR2i and GluR2o respectively, in a calcium influx screening assays.
DC7761	Brincidofovir (CMX-001) Featured	CMX001 (Brincidofovir; HDP-CDV) was developed as an orally active, lipophilic form of cidofovir (CDV); has enhanced activity in vitro and in vivo compared to CDV against certain herpesviruses, adenoviruses and orthopoxviruses.IC50 Value: 5.5 nM (EC50, in PDA at 7 dpi) [3]Target: anti-CMVCMX001 is currently in Phase II clinical studies for development as a therapeutic agent for human CMV, adenovirus and BK virus infections, as well as, for adverse events following smallpox vaccinations.in vitro: In PDA at 7 dpi, the CMX001 50% effective concentration (EC50) was 5.55 nM, the 50% cytotoxic concentration (CC50) was 184.6 nM, and the 50% selectivity index (SI50) was 33.3. The EC90 was 19.7 nM, the CC90 was 5,054 nM, and the SI90 was 256.1. In COS-7 cells, JCV replication was faster and the EC50 and EC90 were 18- and 37-fold higher than those in PDA, i.e., 0.1 μM and 0.74 μM (CC50, 0.67 μM; SI50, 6.7; CC90, 12.2 μM; SI90, 16.5) at 5 dpi [3].in vivo: CMX001 and CDV are equally efficacious at protecting mice from mortality following high ectromelia virus doses (10,000 x LD(50)) introduced by the intra-nasal route or small particle aerosol. Using CMX001 at a 10mg/kg dose followed by 2.5mg/kg doses every other-day for 14 days provided solid protection against mortality and weight loss following an intra-nasal challenge of (100-200) x LD(50) of ectromelia virus [1]. When CMX001 was administered orally to mice infected with HSV-1, mortality was reduced significantly (p≤0.001) with all three dose levels when treatments were initiated 24 h post viral inoculation. When treatments were started 48 h post viral inoculation, 5 and 2.5 mg/kg significantly reduced mortality (p≤ 0.001). If treatments were delayed until 72 h post viral inoculation, CMX001 did not reduce mortality or increase the mean day to death. When mice were infected intranasally with HSV-1 and treatments initiated 24 h post viral inoculation using CMX001 at 5 mg/kg or ACV at 100 mg/kg, virus replication in target organs was reduced by both CMX001 and ACV when compared to vehicle treated mice [2]. Toxicity: Diarrhea was the most common adverse event in patients receiving CMX001 at doses of 200 mg weekly or higher and was dose-limiting at 200 mg twice weekly. Myelosuppression and nephrotoxicity were not observed [4].
DC12476	CN427 Featured	CN427 (CN-427) is novel BRD4 (BD1, 2) inhibitor with IC50 of 66 nM, MV4-11 viability IC50 of 1.1 uM..
DC12477	CN750	CN750 (CN-750) is novel BRD4 (BD1, 2) inhibitor with IC50 of 44 nM, MV4-11 IC50 of 0.54 uM.
DC10752	CNDAC HCl Featured	CNDAC (DFP-10917; TAS-109) is an orally available deoxycytosine nucleoside analog with potential antineoplastic activity.
DC9799	CNDAC Featured	CNDAC is the active component of sapacitabine.
DC9370	CNP-AFU	CNP-AFU (2-Chloro-4-nitrophenyl α-L-fucopyranoside) is a substrate for alpha-L-fucosidase(AFU).
DC10671	CNQX disodium salt Featured	CNQX is a potent AMPA/kainate receptor antagonist. Also antagonist at glycine modulatory site on NMDA receptor complex.
DC10670	CNQX Featured	CNQX is a potent AMPA/kainate receptor antagonist. Also antagonist at glycine modulatory site on NMDA receptor complex.
DC7009	CNS-7056	CNS 7056 is a new short-acting sedative/anaesthetic that acts on GABAA receptors in the brain.
DC20346	CN-SAH	CN-SAH is a potent and selective inhibitor of histone methyl transferase DOT1L with IC50 of 26 nM, displays >10-fold selectivity over DNMT1, PRMT3, PRMT5, and G9α..
DC12103	CNT2 inhibitor-1	CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
DC23180	CNV1014802(Raxatrigine) Featured	CNV1014802 (GSK-1014802, Raxatrigine, Vixotrigine, BIIB074) is a potent, selective Nav1.7 sodium channel blocker, shows analgesic effects and potential in the treatment of cognitive symptoms of schizophrenia in vivo.
DC8095	Raxatrigine hydrochloride Featured	CNV1014802(GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
DC7104	CNX-1351	CNX-1351 is a selective covalent Inhibitor of PI3Kα. CNX-1351 was tested against all four of the class I PI3K enzymes α, β, γ, and δ.
DC7105	CNX-2006 Featured	CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
DC7161	CNX-774 Featured	CNX-774 is a potent, selective, and orally available small molecule inhibitor of Btk (IC50< 1 nM) that forms a ligand-directed covalent bond with Cys-481, a non-conserved amino acid within the active site of the enzyme.
DC8651	CO-1686 hydrobromide Featured	CO-1686 hydrobromide is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M (IC50=21 nM).
DC7106	Rociletinib (CO-1686) Featured	CO-1686 is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M(IC50=21 nM).
DC2046	Cobicistat (GS-9350) Featured	Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

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Inhibitors & Agonists

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