tubulin inhibitor 8

Tubulin inhibitor 8 is an inhibitor of tubulin and various cancer cell lines and inhibits tubulin polymerisation and K562 cell growth with an IC50 of 0.73 μM and 14 nM respectively.

MonomethylauristatinE intermediate-8 is an intermediate compound in the synthesis of MonomethylauristatinE. MonomethylauristatinE (MMAE) acts as a microtubule/tubulin inhibitor with anticancer properties. It is widely utilized as the cytotoxic component in antibody-drug conjugates (ADCs).

EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114 and binds specifically to cysteine 8 (C8) within its intrinsically disordered region, exhibiting an IC50 of 470 nM. EN219 inhibits RNF114-induced autoubiquitination and p21 ubiquitination in cell-free assays at 50 μM. At 1 μM, EN219 interacts with multiple proteins including the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60/HspD1), and histone H3.1 (HIST1H3A) in 231MFP breast cancer cells. Furthermore, EN219 has been linked to the bromodomain inhibitor (+)-JQ1 for the creation of a PROTAC capable of degrading BRD4 in 231MFP cells.

Tubulin polymerization-IN-8 (compound IIc) is a potent inhibitor of tubulin polymerization, inducing concentration-dependent cell cycle arrest at the G2/M phase in HCT116 tumor cells and significantly inhibiting tubulin polymerization with an IC50 of 12.7 μM, showing potential for cancer research [1].

Tubulin/HDAC-IN-3 (compound 12a) is a potent dual inhibitor of tubulin polymerization and HDAC1/8, with IC50 values of 5.4 μM for tubulin polymerization, and 0.155 and 0.177 μM for HDAC1 and HDAC8, respectively. It obstructs the cell cycle, triggers apoptosis, and suppresses colony formation [1].

Colchicine-d6 is a deuterated compound of Colchicine. Colchicine has a CAS number of 64-86-8. Colchicine is a tubulin inhibitor (IC50: 3 nM) and blocks polymerization of microtubules by binding to tubulin.