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Cat. No. Product Name CAS No. Information
PC-60350

ABP-A3

ABP-A3(ABP A3) is an inhibitor of ubiquitin conjugation that targets ubiquitin and Nedd8 E1 enzymes; inhibits conjugation of ubiquitin to intracellular proteins and prevents the formation of cytoprotective aggresomes; induces activation of the unfolded protein response (UPR) and apoptosis, displays IC50 of 2.5 uM in cell viability assays in A549 cells.

PC-60178

TAK-243

1450833-55-2

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.

Solid Tumors

Phase 1 Clinical

PC-43475

PYZD-4409

423148-78-1 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.
PC-43474

PYR-41

418805-02-4 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.
PC-62879

NEDD8 inhibitor M22

864420-54-2 NEDD8 inhibitor M22 is a novel, potent, selective reversible NEDD8 activating enzyme (NAE) inhibitor; inhibit A549 cell proliferation completely at 30 uM (GI50=5.5 uM and GI90=19.3 uM); produces tumor inhibition in AGS xenografts in nude mice and low acute toxicity in zebrafish model; exhibts different binding mode compared with MLN4924.
PC-61698

ML 792

1644342-14-2 ML 792 is a potent, seletive SUMO-activating enzyme (SAE) inhibitor with IC50 of 3 nM and 11 nM for SAE/SUMO1 and SAE/SUMO2, respectively; shows no significant inhibition for closely related E1 enzymes NAE (IC50=32 uM) and ubiquitin-activating enzyme (UAE) (IC50 >100 uM), as well as a panel of 366 ATP-using enzymes; dose-dependently decreases global SUMOylation in HCT116 cells (EC50=19 nM), demonstrates potent antiproliferative effect in HCT116 cells and MDA-MB-231 cells with EC50 of 0.04 and 0.11 uM, respectively.
PC-60355

IJ-5

68776-47-6 A potent, covalent inhibitor of ubiquitin-conjugating enzyme UbcH5 with Kd of 5.189 uM, 3.578 uM, and 2.577 uM for UbcH5a, UbcH5b, and UbcH5c, respectively; shows weak affinity for Ubc13 (Kd=13.37 uM); inhibits TNFα-induced NF-kB pathway activation and inflammatory gene expression in 293T cells, exhibites potent anti-inflammatory activity against TNF-α- and D-galactosamine-induced hepatitis and collagen-induced arthritis in preclinical models.

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