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]}. IC50 & Target:Calcium channel^[1] In Vitro: Carboxyamidotriazole (10 μM; 15 min) suppresses mitochondrial calcium import in Digitonin (HY-N4000)-permeabilized HEK -293 cells^[2].
Carboxyamidotriazole (24 h) inhibits the proliferation of HepG2 and Huh-7 cells, with IC₅₀s of 0.7 μM and 4.5 μM, respectively, as measured by [³H]thymidine incorporation^[3].
Carboxyamidotriazole (10-20 μM; 48 h) dose-dependently inhibits the viability of LLC cells and promotes glucose uptake and lactate production in them^[4].
Carboxyamidotriazole (1-40 μM; 0-5 days) inhibited cell growth in a dose- and time-dependent manner in a proliferation assay of human chronic myeloid leukemia (CML) cell lines (LAMA84R, K562R, KCL22R)^[7].
Carboxyamidotriazole (10-40 μM; pretreatment for 2 h, then co-stimulation with LPS for 6 h) reduced NO production and iNOS expression and downregulated proinflammatory cytokine levels in mouse RAW264.7 macrophages^[8].
Carboxyamidotriazole (5-40 μM, 48 h) inhibited the proliferation of fibroblast-like synoviocytes in a rat adjuvant arthritis model^[9].
Carboxyamidotriazole (1.25-40 μM; 48-72 h) significantly inhibits the proliferation of Lewis lung carcinoma (LLC) cells^[10].
Carboxyamidotriazole (10 μM; 24 h) enhances the cytotoxicity of cytotoxic T lymphocytes (CTLs) and promotes the release of IFN-γ in the co-culture experiment of mouse B16 melanoma cells and CTLs^[12].
In Vivo: Carboxyamidotriazole (30 mg/kg; i.g.; daily; 19 days) combined with 2-deoxyglucose retards the growth of LLC tumors in C57BL/6 mice^[4].
Carboxyamidotriazole (10-40 mg/kg; i.g.; once daily; from day 12 to day 26 after arthritis induction) reduces the severity of arthritis, inhibits hind paw swelling, decreases the infiltration of joint pathological inflammatory cells in the adjuvant arthritis model of Lewis rats induced by complete Freund's adjuvant^[9].
Carboxyamidotriazole (30 mg/kg; i.g.; once daily; from day 7 to day 29 after inoculation of tumor cells) inhibits tumor growth, enhances the weights of gastrocnemius muscle and epididymal adipose tissue in the C57BL/6J mouse model inoculated with Lewis lung carcinoma cells^[10].
Carboxyamidotriazole (30 mg/kg; i.g.; once daily; for 29 days) combined with low-dose Sorafenib (HY-10201) synergistically inhibits tumor growth in the C57BL/6J mouse model inoculated with Lewis lung carcinoma cells^[11].
Carboxyamidotriazole (20 mg/kg; i.g.; once daily) combined with 1-MT or DMF, increases the number of CD8⁺ T cells in tumor-infiltrating lymphocytes (TILs), enhances the anti-tumor immune response of T cells, inhibits tumor growth, and prolongs the survival in the C57BL/6, BALB/c or RAG1 KO mouse models inoculated with B16, C26, 4T1 or B16-OVA tumor cells^[12].
Carboxyamidotriazole (40 mg/kg, p.o., once daily, 14 days) reduces Bleomycin (HY-108345)-induced lung injury in mice^[13].