glutaminase c-in-1

Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C (GLS1).

Ethyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate has an inhibitory effect on coagulation factor Xa, and it can be used in the study of thrombophlebitis, atherosclerosis, cerebral embolism, stroke and pulmonary embolism.

Cyclopenta[c][1]benzopyran-8-ol, 1,2,3,3a,4,9b-hexahydro-4-(4-hydroxyphenyl)-, (3aR,4S,9bS)-rel- is an estrogen receptor beta (ERβ) agonist.

C-Type Natriuretic Peptide (CNP) (1-22), human acetate is an agonist of natriuretic peptide receptor B (NPR-B), an endothelial-derived relaxant and growth inhibitory factor. C-Type Natriuretic Peptide (CNP) (1-22), human acetate inhibits cAMP synthesis stimulated by histamine and 5-HT or directly by Forskolin.

c-Fms-IN-1 is an inhibitor of c-FMS kinase (IC50 = 0.8 nM).

C-Type Natriuretic Peptide (CNP) (1-22), human, is the 1-22 fragment of the parent C-Type Natriuretic Peptide.

c-Met inhibitor 1 is a c-Met receptor signaling pathway inhibitor, used for the treatment of cancer including glioblastoma, gastric, and pancreatic cancer.

C/EBPα inducer 1 (4(3H)-Quinazolinone, 6-fluoro-2-[(1E)-2-(5-nitro-2-furanyl)ethenyl]-3-phenyl-) is a potential inducer of myeloid differentiation via upregulation of C/EBP.

c-Kit-IN-1 (DCC-2618) is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).

Glutaminase C-IN-2 (compound 11), an allosteric inhibitor of glutaminase C (GAC), shows potent inhibitory activity with an IC50 of 10.64 nM. By disrupting glutamine metabolism, it modulates cellular metabolites and elevates reactive oxygen species (ROS), exerting anticancer effects [1].

Glutaminase C Inhibitor 11 is a potent inhibitor specifically targeting Glutaminase C (GAC), demonstrating significant inhibition of GAC enzyme activity with an EC50 value of 10.64 nM. It effectively diminishes the viability of A549 non-small cell lung cancer (NSCLC) cells, presenting an IC50 of 4.025 nM. Moreover, at concentrations of 0.1 and 1 µM, it substantially impedes colony formation and reduces intracellular glutamate levels in A549 cells. Demonstrating efficacy in vivo, Glutaminase C Inhibitor 11 at a dosage of 100 mg/kg markedly curtails tumor growth in an A549 mouse xenograft model.

VEGFR-2 c-Met-IN-1 is a dual inhibitor of VEGFR-2 and c-Met, with IC50 values of 138 nM and 74 nM, respectively, demonstrating antitumor activity [1].

C-Peptide 1 (rat), a β-catenin GSK-3β activator and regulator of the Wnt β-catenin signaling pathway, is utilized in cancer research [1].

NPR-C activator 1 (Compound 1) is a potent agonist (EC50 ~ 1 μM) of natriuretic peptide receptor C (NPR-C), which plays a crucial role in regulating vascular homeostasis, and demonstrates promising in vivo pharmacokinetic properties [1].

c-met-IN-1 is a potent and selective c-Met inhibitor (IC50: 1.1 nM) with antitumor activity.

C-RAF kinase-IN-1 is a potent inhibitor of C-RAF kinase with an IC 50 of 0.193 μM. C-RAF kinase-IN-1 is a quinoline derivative. C-RAF kinase-IN-1 has the potential for the research of cancer diseases .

1-(2-C-b-Methyl-b-D-ribofuranosyl)-5-nitropyridine-2(1H)-one is a Pyridine nucleoside; 2'-C-Methyl nucleoside.

1-b-D-(3-Methoxy naphthalen-2-yl)-2’-deoxyriboside; 1,4-Anhydro-2-deoxy-1-C-(3-methoxy)-naphthalenyl)-D-erythro-pentitol is a useful organic compound for research related to life sciences. The catalog number is TNU1641 and the CAS number is 1117893-19-2.

Dichloro[1,3-bis(2,4,6-trimethylphenyl)-2-imidazolidinylidene][[5-[(dimethylamino)sulfonyl]-2-(1-methylethoxy-O)phenyl]methylene-C]ruthenium(II) is a useful organic compound for research related to life sciences and the catalog number is T66135.

1''-Methoxyerythrinin C is a natural product for research related to life sciences. The catalog number is TN2550 and the CAS number is 221002-11-5.

4-C-(Iodomethyl)-1,2-di-O-(1-methylethylidene)-3,5-bis-O-(phenylmethyl)-a-D-ribofuranose is a Carbohydrate Derivative.

Antiproliferative Against-3 (comp 33) demonstrates significant activity against Hela (IC 50 = 0.21 µM), A549 (IC 50 = 0.39 µM), and MCF-7 (IC 50 = 0.33 µM) cell lines. Additionally, it induces apoptosis in a dose-dependent manner by arresting A549 cells in the G1 phase.

5-O-Benzoyl-4-C-hydroxymethyl-2,3-O-isopropylidene-1-O-methyl-beta-D-ribofuranose is a Carbohydrate Derivative.

4-Fluorobenzo[c][1,2]oxaborol-1(3H)-ol is a useful organic compound for research related to life sciences. The catalog number is T64514 and the CAS number is 174671-88-6.

threo-1-C-Syringylglycerol is a natural product for research related to life sciences. The catalog number is TN5143 and the CAS number is 121748-11-6.

Formononetin-8-C-beta-D-apiofuranosyl-(1->6)-O-beta-D-glucopyranoside is a natural product for research related to life sciences. The catalog number is TN6636 and the CAS number is 1147858-78-3.

4-Chloro-1-(2-methylpropyl)-1H-imidazo[4,5-c]quinoline is a useful organic compound for research related to life sciences. The catalog number is T65458 and the CAS number is 99010-64-7.

1-(2,3,5-Tribenzoyl-2-C-b-methyl-b-D-ribofuranosyl)-5-nitropyridine-2(1H)-one is a Pyridine nucleoside; 2'-C-Methyl nucleoside.

1-alpha-D-(3-Meth oxynaphthalen-2-yl)-2’-deoxy riboside; (1S)-1,4-Anhy dro-2-deoxy-1-C-(3-methoxy)-naphthalenyl)-D-erythro-pentitol is a useful organic compound for research related to life sciences. The catalog number is TNU1648 and the CAS number is 1502811-53-1.

Beta-D-homoDNA-C(Bz)-phosphorami dite; N4-Benzoyl-1-[6-O-DMTr-2,3-dideoxy-4-(O-CED-phosphoramitidyl)-beta-D-erythro-hexopyranosyl)cytosine is a useful organic compound for research related to life sciences and the catalog number is TNU1624.

1',2'-Di-O-acetayl-3',5'-di-O-benzoyl-3'-beta-C-ethynyl-D-ribofuranose is a carbohydrate derivative.

Ethyl 1-(4-methoxyphenyl)-6-(4-nitrophenyl)-7-oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate is a useful organic compound for research related to life sciences. The catalog number is T66226 and the CAS number is 536759-91-8.

PAF C-18:1 is a naturally occurring phospholipid produced by cells upon stimulation and plays a role in the establishment and maintenance of the inflammatory response. It is less potent than PAF C-16 and PAF C-18 in the induction of neutrophil chemotaxis, but is equipotent to PAF C-16 and PAF C-18 in promoting eosinophil migration. PAF C-18:1 activates the PAF receptor and has been used in antibody binding experiments to determine the importance of an acyl linkage at the sn-2 position for recognition at this receptor.

3-(6-Chloro-1-oxo-1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-yl)piperidine-2,6-dione is a useful organic compound for research related to life sciences and the catalog number is T64655.

Drugs and Inhibitors; toll-like receptor (TLR) agonist

C-Type Natriuretic Peptide (CNP) (1-22), human (TFA), is a 22 amino acid fragment of CNP that functions as an agonist for the natriuretic peptide receptor B (NPR-B). It can inhibit cAMP synthesis induced by histamine, 5-HT, or Forskolin, while exhibiting strong endothelial-derived relaxation properties and acting as a growth inhibitor.

(1S)-1,4-Anhydro-1-C-(2,4-difluorophenyl)-D-ribitol is a nucleoside derivative, specifically a C-nucleoside with fluoro modifications.

1-O-Acetyl-2,3,5-tri-O-benzoyl-5(R)-C-methyl-D-ribofuranose is a carbohydrate derivative.

4-Amino-5-cyano-1-(2-β-C-methyl-β-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine, a purine nucleoside analogue, exhibits widespread antitumor efficacy, particularly against indolent lymphoid malignancies. Its anticancer properties primarily stem from the inhibition of DNA synthesis and the induction of apoptosis, among other mechanisms [1].

1-(2'-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is a bicyclic nucleoside.

(1S)-1,4-Anhydro-1-C-(2,4-difluoro-5-methylphenyl)-D-ribitol is a nucleoside derivative, specifically a C-nucleoside, modified with fluorine (fluoro-modified nucleoside).

1',2',3',5'-Tetra-O-benzoyl-2'-beta-C-ethynyl-D- ribofuranose is a carbohydrate derivative.

4-Amino-1-(2-b-C-methyl-b-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine-5-carboxamide is a Nucleoside Derivative - 7-Deaza-purine nucleoside; 2'-Modified nucleoside.

Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate p

MEK1 C-Raf-IN-1 (Compound 14d) serves as an inhibitor of MEK1 and C-Raf, exhibiting IC50 values of 97 nM and 23 nM, respectively. It also displays antitumor activity [1].

PARP1 c-Met-IN-1 (Compound 16) serves as a selective dual inhibitor targeting both PARP1 and c-Met, demonstrating IC50 values of 3.3 nM and 32.2 nM, respectively. This compound effectively induces apoptosis and causes cell cycle arrest at the G2 M phase in MDA-MB-231 cells. Furthermore, PARP1 c-Met-IN-1 displays notable antitumor activity in mouse models [1].

Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine inhibitor of the renal-type glutaminase (KGA) variant, exhibited antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model.