vinblastine

Vinblastine inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM, used to treat certain kinds of cancer.

Vinblastine sulfate (Vincaleukoblastine sulfate salt) can inhibit the formation of microtubule, it also inhibits nAChR(IC50=8.9 uM).

MC-Val-Cit-PAB-vinblastine is a potent antitumor drug-linker conjugate for Antibody-Drug Conjugates (ADC), featuring vinblastine (a microtubule protein inhibitor) connected through the MC-Val-Cit-PAB [ADC linker].

Desacetylvinblastine (4-Desacetylvinblastine) is a primary metabolite of vinblastine and functions as a cytotoxic agent. While its antitumor efficacy is limited when used alone, it can exhibit significant antitumor activity when involved as part of specific conjugates.

Deacetylvinblastine hydrazide, a cytotoxic vinca alkaloid often conjugated with folic acid to produce EC145, a novel folate-receptor targeted agent.

3', 4'-Anhydrovinblastine (3',4'-Anhydrovinblastine) is an antineoplastic agent.

Cevipabulin (TTI-237) is a microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin (IC50: 18-40 nM in the human tumor cell line).

Pristinamycin IA (Mikamycin B) is a cyclo-peptidic macrolactone antibiotic and a substrate for the P-glycoprotein.

ALB-109564 dihydrochloride is a semi-synthetic derivative of the vinka alkaloid vinblastine with potential antineoplastic activity, a microtubule protein inhibitor and antineoplastic compound. It binds to tubulin monomers and inhibits microtubule formation, resulting in disruption of mitotic spindle assembly and arrest of tumor cells in the G2/M phase of the cell cycle.

Cevipabulin (TTI-237) fumarate is a microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin (IC50: 18-40 nM in the human tumor cell line).

Vindesine sulfate (Desacetyl Vinblastine amide) is a vinca alkaloid which is a synthetic derivative of vinblastine, binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death.

Torilin is an inhibitor of testosterone 5 alpha-reductase, it (IC50 = 31.7 + - 4.23 microM) shows a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3 + - 24.62 microM) but is weaker than finasteride (IC50 = 0.38 + - 0.06 microM). Torilin has immunomodulatory, hepatoprotective, and anti-inflammatory properties, it inhibits inflammation by limiting TAK1-mediated MAP kinase and NF-κB activation, it can attenuate arthritis severity, modify leukocyte activations in dLNs or joints, and restore serum and splenocyte cytokine imbalances. Torilin inhibits melanin production in alpha-melanocyte stimulating hormone-activated B16 melanoma cells, with an IC(50) value of 25 microM. Torilin shows excellent antimicrobial activity against Bacillus subtilis ATCC 6633 spores and vegetative cells. Torilin has a potent anti-angiogenic activity both in vivo and in vitro, and it may have a strong activity to suppress tumorigenesis by inhibition of tumor invasion, it reverses multidrug-resistance in cancer cells, it can potentiate the cytotoxicities of adriamycin, vinblastine, taxol and colchicine against multidrug-resistant KB-V1 and MCF7 ADR cells.

Migrastatin is a bacterial metabolite that has been found inStreptomyceswith antimuscarinic and anticancer activities.1,2It binds to M1-5muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 μM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50= 28 μM), as well as in primary rat bladder smooth muscle cells.1Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50= 10 μg/ml) and 4T1 mouse mammary carcinoma cells in a chamber cell migration assay (IC50= 29 μM).2It enhances cytotoxicity induced by vinblastine in vincristine-resistant P388/VCR cells.3

C2 Adamantanyl globotriaosylceramide (AdaGb3) is a bioactive sphingolipid and water-soluble form of globotriaosylceramide that contains an adamantanyl group in place of the fatty acyl chain. It inhibits Vero toxin binding to globotriaosylceramide in an ELISA assay when used at a concentration of 10 μM. AdaGb3 decreases cell surface expression of P-glycoprotein (P-gp) and reduces efflux of rhodamine 123 in MDCK cells. It also increases apical-to-basal transport of vinblastine in human intestinal C2BBe1 cells.

BE-10988 is a DNA topoisomerase (DNAtopoisomerase) inhibitor. It suppresses the growth of P388 murine leukemia cell lines that are resistant to Doxorubicin and Vinblastine by promoting the formation of DNA topoisomerase complexes.

Avanbulin is a potent inhibitor of tubulin polymerization with antitumor activity. It elicits a unique microtubule (MT) phenotype, distinct from colchicine, paclitaxel, and vinblastine has broad in vitro anti-proliferative activity against a diverse range

EC0489 is a small molecule-drug conjugate (SMDC) that combines folic acid and desacetyl vinblastine hydrazide, serving as a high-affinity ligand for the folate receptor (FR) in refractory or metastatic tumors.

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4 SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

Isotenulin inhibits the efflux function of P-glycoprotein (P-gp) by stimulating P-glycoprotein ATPase, helping to overcome multidrug resistance (MDR) in cancer cells. It exhibits cytotoxicity in multidrug-resistant cancer cells KB-vin and in sensitive cancer cells HeLaS3. Additionally, Isotenulin acts synergistically with Paclitaxel, Vinblastine, and Doxorubicin.

CCK2R Ligand-Linker Conjugate 1 is a hydrophilic peptide linker that conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) as ligand-linker conjugates[1].

Inhibitor of microtubule polymerization in vitro. Interacts with tubulin dimers and promotes the accumulation of mammalian cells in apoptosis. Potentiates antiproliferative effects of vinblastine in H2B-GFP HeLa cells. Originally thought to inhibit CENP-E ATPase activity. Tcherniuk et al (2011) UA62784 is a cytotoxic inhibitor of microtubules, not CENP-E. Chem.Biol. 18 631 PMID:21609844 |Maiato and Logarinho et al (2011) Motor-dependent and -independent roles of CENP-E at kinetochores: the cautionary tale of UA62784. Chem.Biol. 18 679 PMID:21700202

A 30312 is a fused indole, which overcomes multidrug resistance in P388/Adr cells in vitro. It potentiates the cytotoxicity of the antitumor drugs Adriamycin, vincristine and vinblastine in multidrug-resistant cells with no effect on drug-sensitive parent P388 cells.

Odorine has potent anti-carcinogenic effect by inhibiting both the initiation and promotion stages of two-stage skin carcinogenesis. It was found to inhibit the growth of the vinblastine-resistant KB cells by enhancing the anticancer activity of vinblastine.