Thiocolchicoside

Thiocolchicoside is a GABAA receptor antagonist. It inhibits GABAA receptor-mediated currents in Purkinje cells isolated from rat cerebellum (IC50 = 0.15 µM). It binds strychnine-sensitive glycine receptors in isolated rat spinal cord (IC50 = 1.58 µM). Thiocolchicoside inhibits cell growth in a panel of cancer cell lines, including KBM5 leukemia and U266 myeloma cells, SCC4 squamous cell carcinoma cells, and HCT116 colon, MCF-7 breast, and A293 kidney cancer cells when used at concentrations ranging from 25 to 100 µM. It inhibits the anti-apoptotic proteins Bcl-2, X-linked inhibitor of apoptosis (XIAP), myeloid cell leukemia-1 (Mcl-1), Bcl-xL, cIAP-1, and cIAP-2 in KBM5 cells in a concentration-dependent manner. It also inhibits TNF-alpha-induced NF-kappaB activation and IkappaBalpha degradation in KBM5 cells in a concentration-dependent manner. Formulations containing thiocolchicoside have been used as muscle relaxers in the treatment of rheumatoid arthritis, joint stiffness, and muscle stiffness.Formal Name: N-[(7S)-3-(beta-D-glucopyranosyloxy)-5,6,7,9-tetrahydro-1,2-dimethoxy-10-(methylthio)-9-oxobenzo[a]heptalen-7-yl]-acetamide. CAS Number: 602-41-5. Synonyms: NSC 147755, R-271. Molecular Formula: C27H33NO10S. Formula Weight: 563.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: 5 mg/ml, Ethanol: insol, PBS (pH 7.2): 5 mg/ml. lambdamax: 257, 291, 382 nm. SMILES: COC1=C2C(C([C@H](CCC2=CC(O[C@@H]3O[C@@H]([C@H]([C@@H]([C@H]3O)O)O)CO)=C1OC)NC(C)=O)=C4)=CC=C(SC)C4=O. InChi Code: InChI=1S/C27H33NO10S/c1-12(30)28-16-7-5-13-9-18(37-27-24(34)23(33)22(32)19(11-29)38-27)25(35-2)26(36-3)21(13)14-6-8-20(39-4)17(31)10-15(14)16/h6,8-10,16,19,22-24,27,29,32-34H,5,7,11H2,1-4H3,(H,28,30)/t16-,19+,22+,23-,24+,27+/m0/s1. InChi Key: LEQAKWQJCITZNK-AXHKHJLKSA-N.