Carboxyamidotriazole

Carboxyamidotriazole (L-651582) is an orally active cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole inhibits NF-κB, MAPK activation and NO production. Carboxyamidotriazole has anti-angiogenic and anti-inflammatory activities. Carboxyamidotriazole has anticancer activity against liver cancer, lung cancer and leukemia[1][2][3][4][5][6][7][8][9][10][11][12][13].

Product Specifications

CAS Number

[99519-84-3]

Product Name Alternative

L-651582; CAI

UNSPSC

12352005

Hazard Statement

H301

Target

Calcium Channel; NF-κB; NO Synthase; p38 MAPK

Type

Reference compound

Related Pathways

Immunology/Inflammation; MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Neuronal Signaling; NF-κB

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/carboxyamidotriazole.html

Purity

99.32

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=C(N)N(CC2=CC(Cl)=C(C(C3=CC=C(Cl)C=C3)=O)C(Cl)=C2)N=N1)N

Molecular Formula

C17H12Cl3N5O2

Molecular Weight

424.67

Precautions

H301

References & Citations

[1]Hussain MM, et al. J Clin Oncol. 2003 Dec 1;21 (23) :4356-63.|[2]Mignen O, et al. Carboxyamidotriazole-induced inhibition of mitochondrial calcium import blocks capacitative calcium entry and cell proliferation in HEK-293 cells. J Cell Sci. 2005 Dec 1;118 (Pt 23) :5615-23.|[3]Enfissi A, et al. The blocking of capacitative calcium entry by 2-aminoethyl diphenylborate (2-APB) and carboxyamidotriazole (CAI) inhibits proliferation in Hep G2 and Huh-7 human hepatoma cells. Cell Calcium. 2004 Dec;36 (6) :459-67. |[4]Ju R, et al. Carboxyamidotriazole inhibits oxidative phosphorylation in cancer cells and exerts synergistic anti-cancer effect with glycolysis inhibition. Cancer Lett. 2016 Jan 28;370 (2) :232-41.|[5]Faehling M, et al. Essential role of calcium in vascular endothelial growth factor A-induced signaling: mechanism of the antiangiogenic effect of carboxyamidotriazole. FASEB J. 2002 Nov;16 (13) :1805-7.|[6]Bonnefond ML, et al. Inhibition of store-operated channels by carboxyamidotriazole sensitizes ovarian carcinoma cells to anti-BclxL strategies through Mcl-1 down-regulation. Oncotarget. 2018 Sep 21;9 (74) :33896-33911.|[7]Alessandro R, et al. Effects of carboxyamidotriazole on in vitro models of imatinib-resistant chronic myeloid leukemia. J Cell Physiol. 2008 Apr;215 (1) :111-21.|[8]Lu S, et al. Carboxyamidotriazole exerts anti-inflammatory activity in lipopolysaccharide-induced RAW264.7 macrophages by inhibiting NF-κB and MAPKs pathways. Exp Ther Med. 2020 Aug;20 (2) :1455-1466.|[9]Zhou Y, et al. Carboxyamidotriazole alleviates pannus formation and cartilage erosion in rats with adjuvant arthritis. Heliyon. 2023 Sep 14;9 (9) :e20105.|[10]Chen C, et al. Carboxyamidotriazole alleviates muscle atrophy in tumor-bearing mice by inhibiting NF-κB and activating SIRT1. Naunyn Schmiedebergs Arch Pharmacol. 2017 Apr;390 (4) :423-433. |[11]Chen C, et al. Carboxyamidotriazole Synergizes with Sorafenib to Combat Non-Small Cell Lung Cancer through Inhibition of NANOG and Aggravation of Apoptosis. J Pharmacol Exp Ther. 2017 Aug;362 (2) :219-229. |[12]Shi J, et al. Carboxyamidotriazole combined with IDO1-Kyn-AhR pathway inhibitors profoundly enhances cancer immunotherapy. J Immunother Cancer. 2019 Sep 11;7 (1) :246. |[13]Tao Z, et al. Therapeutic effect and mechanism of carboxyamidotriazole on the pulmonary fibrosis of mice induced by bleomycin. Zhonghua Yi Xue Za Zhi. 2018 Feb 27;98 (8) :612-616. Chinese.