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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC78875 MCB-294
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer.
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DC78874 5-cis-15(R)-Iloprost
5-cis-15(R)-Iloprost (5-cis-15(R)-Ciloprost) is the C-5 cis-isomer and 15(R)-epimer of Iloprost. Iloprost is a prostacyclin (PGI2) analogue, involves in embryo development and inflammation improvement, and inhibits tumor metastasis. Iloprost can be used for peripheral vascular research.
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DC78873 BMS-199264
BMS-199264 is an inhibitor of F1F0 ATP hydrolase (IC50=0.5 μM) without inhibitory effect on F1F0 ATP synthase. BMS-199264 selectively inhibits ATP decline during ischemia to reduces cardiac necrosis. BMS-199264 also enhances the recovery of contractile function following reperfusion.
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DC78872 D-myo-Inositol-1,2,4,5,6-pentaphosphate sodium salt
D-myo-Inositol-1,2,4,5,6-pentaphosphate (Ins(1,2,4,5,6)P5) sodium salt is one of several different inositol oligophosphate isomers involved in signal transduction. In human Jurkat T lymphocytes, Ins(1,2,4,5,6)P5 (sodium salt) is phosphorylated to InsP6 by 1/3 kinase. D-myo-Inositol-1,2,4,5,6-pentaphosphate sodium salt is involved in calcium signaling.
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DC78871 2-NH2-PuTP sodium
2-NH2-PuTP (n2h6ATP) sodium, an ATP analogue, is a competitive pyruvate-stimulated adenylate cyclase inhibitor with a Ki of 1.7 mM.
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DC78870 COPCP trisodium
COPCP trisodium (Compound 7a) is a potent and selective ecto-5'-nucleotidase CD73 inhibitor. COPCP trisodium blocks CD73-mediated adenosine production, reducing the inhibitory effect of adenosine on immune cells. COPCP trisodium is promising for research of cancers.
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DC78869 HCA-6
HCA-6 is a calcium-channel and P-glycoprotein blocker. HCA-6 can induce cancer cells apoptosis and increase anticancer activity of Cisplatin. HCA-6 also exhibits antibacterial activity against Bacillus subtilis. HCA-6 can be used for the research of cancer and infection, such as breast cancer.
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DC78868 5'-Amino-5'-deoxyuridine
5'-Amino-5'-deoxyuridine is a nucleoside analog that can be used in nucleic acid synthesis.
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DC78867 CP-283097
CP-283097 is a conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors.
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DC78866 (GalNAc)3-CPT
(GalNAc)3-CPT is a glycoconjugate prodrug that targets the asialoglyco-protein receptor (ASGR) overexpressed on hepatocytes. (GalNAc)3-CPT exhibits significant antitumor activity (IC50 value of 3.07 μM in HepG2 cells) by activating the cGAS-STING pathway and promoting CD8+ T cell infiltration into tumors, thereby inducing tumor cell apoptosis.
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DC78865 Ganglioside GT1b
Ganglioside GT1b is a member of the ganglioside family. Ganglioside GT1b acts as a protective signal against nerve injury-induced spinal synapse elimination. Ganglioside GT1b induces HA synthesis and the phosphorylation of Akt/mTOR in orbital fibroblasts. Ganglioside GT1b enhances porcine oocyte maturation and induce activation of EGFR and ERK1/2 signaling. Ganglioside GT1b is a putative host cell receptor for the Merkel cell polyomavirus. Ganglioside GT1b can be used for the researches of cancer, infection, immunology, endocrinology and neurological disease, such as Thyroid eye disease.
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DC78864 D-myo-Inositol-1,2,3,5-tetraphosphate tetrasodium
D-myo-inositol-1,2,3,5-tetraphosphate (Ins(1,2,3,5,6)-P5) tetrasodium is one of the Inositol phosphate isomers and can act as a soluble second messenger to participate in cellular calcium signaling.
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DC78863 D-myo-Inositol-1,2,4,5-tetraphosphate tetrasodium salt
D-myo-Inositol-1,2,4,5-tetraphosphate (DL-Ins-(1,2,4,5)P4) tetrasodium is raracemic regioisomer of myo-inositol tetrakisphosphates (IP4s). D-myo-Inositol-1,2,4,5-tetraphosphate tetrasodium is an Ins(1,4,5)P3 receptor agonist with a Ki of 11 nM. D-myo-Inositol-1,2,4,5-tetraphosphate tetrasodium induces Ca2+ mobilization with an EC50 value of 0.22 μM in CHO cells.
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DC78862 Glycerophosphoinositol 4,5-diphosphate trisodium
Glycerophosphoinositol 4,5-diphosphate (GroPI(4,5)P2) trisodium is a slowly metabolized analog of InsP3. Glycerophosphoinositol 4,5-diphosphate trisodium has an EC50 of 1.228 μM for inducing calcium release, with a degradation time constant of 13 seconds. Glycerophosphoinositol 4,5-diphosphate trisodium can be used to study the effect of InsP3 degradation on calcium signal recovery.
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DC78861 Glycerophosphoinositol 4-phosphate disodium
Glycerophosphoinositol 4-phosphate (GroPIns-4-P) disodium is a metabolite of phospholipase A and an inhibitor of adenylylcyclase. Glycerophosphoinositol 4-phosphate disodium can regulate cAMP-dependent cellular functions. Glycerophosphoinositol 4-phosphate disodium can also induce the formation of membrane ruffles and stress fibers in serum-starved Swiss 3T3 cells by activating the small GTPases Rac and Rho, respectively. Glycerophosphoinositol 4-phosphate disodium can be used in research on cancer cell motility and invasiveness.
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DC78860 APG-7
APG-7 binds to the TLR4/MD-2 interface, thereby inhibiting NO production (IC50 of 24.2 μg/mL). APG-7 is an Apigenin derivative. APG-7 has low toxicity to the 3T3 fibroblast cell line. APG-7 can be used for the study of oxidative stress and inflammation.
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DC78859 NIP-121
NIP-121 is a new type of potassium channel opener. NIP-121 significantly reduces mean pulmonary artery pressure and total pulmonary resistance through vasodilation. NIP-121 can be used for research on pulmonary arterial hypertension.
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DC78858 D-myo-Inositol-1,3,4,5,6-pentaphosphate ammonium salt
D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) (Ins(1,3,4,5,6)P5 (ammonium salt)) is an isomer of inositol phosphate that acts as a small and soluble second messenger in the transmission of cellular signals. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) can bind to the PH domain of Grp1 with a Kd of 590 nM. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) can inhibit the phosphorylation and kinase activity of Akt/PKB, inducing apoptosis in ovarian, lung, and breast cancer cells. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) exhibits antiangiogenic activity in vitro and blocks capillary tube formation of HUVEC. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) exerts antitumor effects against cancer xenografts in nude mice.
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DC78857 Tauroursocholic acid sodium
Tauroursocholic acid (TUCA) sodium is a taurine-conjugated form of the bile acid ursocholic acid and the 7β-hydroxy epimer of Taurocholic acid. Tauroursocholic acid sodium exists in abundance during the biliary tract cancer, disrupting the balance and cellular toxicity of bile acids and inducing carcinogenesis through oxidative DNA damage and DNA mutation. Tauroursocholic acid (TUCA) sodium can be used for biliary tract cancer research.
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DC78856 R 116712
R 116712 is a highly selective and affinity 5-HT4 receptor ligand. R 116712 can prepare isotopic markers.
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DC78855 Naxaprostene
Naxaprostene is a prostacyclin analogue. Naxaprostene was much more selective for IP receptors and tended towards partial agonism. Naxaprostene inhibits ADP-induced platelet aggregation. It has been shown to prevent rabbit carotid artery thrombosis.
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DC78854 7-MAD-MDCPT-AC-(s-cyclopropane)
7-MAD-MDCPT-AC-(s-cyclopropane) is a derivative of camptothecin. 7-MAD-MDCPT-AC-(s-cyclopropane) can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. 7-MAD-MDCPT-AC-(s-cyclopropane) can be used for cancer research.
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DC78853 AR-102
AR-102 has inhibitory activity towards Staphylococcus aureus. AR-102 exhibits a competitive potent inhibition of the F98Y mutant DHFR (Ki = 0.22 nM). AR-102 has been determined as ternary complex with NADPH in both wild-type S. aureus DHFR and the TMP-resistant F98Y mutant enzyme.
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DC78852 AR-102 isopropyl ester
AR-102 isopropyl ester is a second-generation prostaglandin FP agonist. AR-102 isopropyl ester can be studied in research for glaucoma and ocular hypertension.
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DC78851 (S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide
(S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide (compound 4) is a STING agonist containing a key amide benzimidazole (ABZI) component and shows reproducible inhibition of 3H-cGAMP binding to STING with an apparent inhibition constant IC50 of 14 μM. (S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide can be used for tumor research.
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DC78849 N-Di(D-mannose)-PEG12-MC-VC-PAB-MMAE
N-Di(D-mannose)-PEG12-MC-VC-PAB-MMAE is a linker that can be synthesized to antibody-drug conjugate (ADC). N-Di(D-mannose)-PEG12-MC-VC-PAB-MMAE can be used for the study of cancer.
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DC78846 Crovozalpon
Crovozalpon (Compound 4) is an inhibitor of alplha-1-antitrypsin. Crovozalpon can be used as a prodrug. Crovozalpon can be studied in research for diseases associated with alplha-1-antitrypsin
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DC78845 GCS-12–6
GCS-12–6 is a potent Th2-selective NKT cell agonist targeting CD1d protein. GCS-12–6 is promising for research of autoimmune diseases (e.g., inflammatory bowel disease, multiple sclerosis).
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DC78844 ASI-222
ASI-222 is an aminosugar cardiac glycoside. ASI-222 can inhibit Na+/K+ ATPase and show positive inotropic effect. ASI-222 can be used for the research of cardiovascular disease.
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DC78843 EC-0225
EC-0225, a folate conjugate of two agents- one a potent microtubule inhibiting agent, and the second a DNA alkylating agent. EC-0225 inhibits the growth of folate receptor (FR)-positive KB cells with an IC50 of ~1 nM. EC-0225 can be selectively delivered to advanced FR-positive tumors without causing overt toxicity, such as lung carcinoma.
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