| Cat. No. |
Product Name |
CAS No. |
Information |
| GY04418 |
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. |
| GY02830 |
PD150606
|
179528-45-1 |
A potent and selective calpain inhibitor with Ki of 0.21 uM/0.37 uM for u-calpain/m-calpain, respectively; shows no inhibition for other proteases (cathepin B, papain, trypsin and thermolysin (Ki> 500 uM); attenuate shypoxic/hypoglycemic injury to cerebrocortical neurons in culture and excitotoxic injury to Purkinje cells in cerebellar slices. |
| GY02709 |
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. |
| GY07020 |
FV-162
|
1565822-28-7 |
FV-162 is a potent, orally bioavailable, irreversible proteasome inhibitor with potent antimyeloma activity (IC50<60 nM); induces rapid, irreversible inhibition of chymotrypsin-like proteasome activity in murine red blood cells and inhibits tumor growth in myeloma xenograft model. |
| GY10174 |
KZR-616
|
1629677-75-3 |
KZR-616 (KZR616) is a potent, selective dual immunoproteasome subunit LMP7/LMP2 inhibitor with IC50 of 39 nM/139 nM, weakly inhibits β5, MECL-1 and no acitivty against β1 subunit; shows no inhibition at 10 uM against a broad selectivity panel of 20 serine, metallo-, cysteine and aspartyl proteases and 11 hydrolases; demonstrates efficacy in the anti-collagen antibody induced arthritis (CAIA) models. |
| GY02292 |
MLN9708
|
1239908-20-3 |
A potent, selective, orally bioavailable proteasome inhibitor with IC50 of 3.4 nM; binds to and inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with Ki of 0.93 nM, weakly inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50 of 31 and 3,500 n M); inhibits growth and induces apoptosis in MM cells; shows improved antitumor activity in models of lymphoma compared with bortezomib. |
| GY01911 |
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. |
| GY04196 |
VR-23
|
1624602-30-7 |
A potent inhibitor of trypsin-like proteasome (IC50=1 nM), chymotrypsin-like proteasome (IC50=50-100 nM) and caspase-like proteasome (IC50=3 uM); targets the β2 of the 20S proteasome catalytic subunit and structurally distinct from other known proteasome inhibitors and selectively kills cancer cells by apoptosis, with little effect on noncancerous cells. |
| GY01670 |
MG-101
|
110044-82-1 |
MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki= 190 nM), calpain II (Ki= 220 nM), cathepsin B (Ki= 150 nM) and cathepsin L (Ki= 500 pM); activates p53-dependent apoptosis in tumor cell lines; increases activated p53, p21 and caspase levels and promotes cell cycle arrest through inhibition of cyclin D degradation in vitro. |
| GY01604 |
Delanzomib
|
847499-27-8 |
Delanzomib is a potent, orally active proteasome inhibitor with IC50 of 3.8 nM against chymotrypsin-like proteasome activity; demonstrates marginal inhibition of the tryptic and peptidyl glutamyl activities of the proteosome; down-modulates the NF-kappaB activity and the expression of several NF-kappaB downstream effectors, induces apoptotic cell death in MM cells; demonstrates tumor regression in MM xenografts with favorable tumor selectivity profile. |
$ USD
Select Your Country or Region
