| Cat. No. |
Product Name |
CAS No. |
Information |
| H9428 |
ACU-D1
|
26347-98-8 |
ACU-D1 is a First-in-Class, novel,efficacy and safety inhibitor of the 26S protea-some for the treatment of moderate to severe rosacea. |
| H7288 |
UK-101
|
1000313-40-5 |
A potent, specific immunoproteasome β1i (LMP2) subunit inhibitor with IC50 of 104 nM, 144- and 10-fold selectivity over β1c and β5 subunit respectivey; induces apoptosis of PC-3 cells and results in significant inhibition (~50-60%) of tumour growth in vivo, does not block degradation of IκBα in PC-3 cells treated with TNF-α. |
| H7287 |
TCH-165
|
1446350-60-2 |
TCH-165 is a specific small molecule modulator of proteasome assembly, regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation; enhances the degradation of both α-syn and tau, does not induce the degradation of GAPDH, enhances the degradation of intrinsically disordered proteins in cell culture; display a decrease in assembled 26S and an increase in 20S proteasome in treated cells. |
| H7286 |
Rpn11 inhibitor 35
|
2084868-04-0 |
Rpn11 inhibitor 35 is a potent, small molecule inhibitor of the proteasome subunit Rpn11 with IC50 of 400 nM,100-fold selectivity over Csn5 and 10-fold selectivity over AMSH; inhibits 293T and A549 cells proliferation with IC50 of 2.1 and 3.8 uM, respectively. |
| H7285 |
RA190
|
1617495-03-0 |
RA190 (RA-190)?is a reversible, highly selective, orally active inhibitor of the proteasomal ubiquitin receptor Rpn13, exhibits potent anti-proliferative effects against MM lines (IC50<0.1 uM) and HPV-transformed cells (IC50<0.3 uM); inhibits proteasome function, triggering rapid accumulation of polyubiquitinated proteins; profoundly reduced growth of MM and ovarian cancer xenografts. |
| H7284 |
PR-924
|
1416709-79-9 |
A potent, specific immunoproteasome LMP7 subunit inhibitor with IC50 of 25 nM, >100-fold selectivity over β5c, β1i, β1c, β2i and β2c subunits (IC50>3 uM); shows weak activity toward LMP2 and no detectable activity toward β1, β2, or MECL1. |
| H7283 |
PR-893
|
1426305-23-8 |
A potent, specific immunoproteasome β5 subunit inhibitor with IC50 of 17 nM, 21-fold and 13-fold selectivity for β5 over LMP7 and LMP2 subunits, respecitvely. |
| H7282 |
PR-825
|
935888-08-7 |
A potent, specific immunoproteasome β5 subunit inhibitor. |
| H7281 |
PI-1840
|
1401223-22-0 |
PI-1840 is a potent, selective, noncovalent, reversible inhibitor for proteasome chymotrypsin-like (CT-L) activity with IC50 of 27 nM, shows no effect on trypsin-like and peptidylglutamyl peptide hydrolyzing activities (IC50>100 uM); also displays 100-fold more selectivity for the constitutive proteasome over the immunoproteasome; induces the accumulation of proteasome substrates p27, Bax, and IκB-α, inhibits survival pathways and viability, and induces apoptosis in intact cancer cells, also sensitizes human cancer cells to the mdm2/p53 disruptor Nutlin; suppresses the growth in nude mice of human breast tumor xenografts. |
| H7280 |
PD-151746
|
179461-52-0 |
A potent, selective, cell-permeable Calpain inhibitor with Ki of 0.26 uM for m-calpain; displays 20-fold selectivity over m-calpain; attenuates the SLLVY-AMC hydrolysis induced by maitotoxin in SY5Y cells; decreases cytotoxicity induced by oxidized low-density lipoprotein (oxLDL) in HMEC-1 cells. |
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