|Cat. No.||Product Name||CAS No.||Information|
COH000 (COH-000) is a highly selective, first-in-class, irreversible, allosteric, covalent inhibitor of SUMO-Activating Enzyme E1, inhibits SUMOylation in vitro with IC50 of 0.2 uM, displays >500-fold selectivity for SUMOylation over ubiquitylation; increased the degradation of SAE2, increases the expression of miR-34b and reduces c-Myc levels in lymphoma and colorectal cancer cell lines and a colorectal cancer xenograft mouse model.
PYZD-4409 is a specific inhibitor of ubiquitin-activating enzyme (E1) with IC50 of 20 uM, inhibits the ATP-dependent activation of ubiquitin and subsequent transfer of the activated ubiquitin from the E1 to the common human E2 enzyme UBE2E2; blockes the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc3, induces cell death in hematologic malignant cell lines and primary patient samples preferentially over normal hematopoietic cells; decreases tumor weight and volume without untoward toxicity in vivo.
TAK-243 (MLN-7243, AOB87172) is a small-molecule, cell-permeable inhibitor of ubiquitin-activating enzyme E1 (UAE1); blocks ssential monoubiquitination events within the translesion synthesis, and homologous recombination (HR) pathways; shows synergistic and additive anti-tumor combination benefits in vivo combined with carboplatin and docetaxel.
PYR-41 is a selective, cell-permeable inhibitor of ubiquitin-activating enzyme (E1), blocks loading of immobilized His6-tagged E1 with ubiquitin with IC50 of <10 uM; does not affect the transfer of ubiquitin to E2 from E1, directly inhibits E1, but not E2; in addition to blocking ubiquitylation, PYR-41 increases total sumoylation in cells, attenuates cytokine-mediated nuclear factor-kappaB activation and inhibits nonproteasomal (Lys-63) ubiquitylation of TRAF6, also prevents the downstream ubiquitylation and proteasomal degradation of IκBα; inhibits degradation of p53 and activates the p53 transcriptional activity, demonstrates anti-tumor activity in animal studies.
No.1378 West Wenyi Road, Yuhang District, HangZhou, Zhejiang, China