Zetomipzomib (KZR-616) maleate is a first-in-class inhibitor of immunoproteasome that selectively targets the immunoproteasome subunit LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50:131/179 nM=hLMP7/mLMP7). Potential of Zetomipzomib maleate for use in multiple autoimmune diseases.
|Solubility (25°C)||DMSO ≥ 200 mg/mL|
|Storage||2-8℃, dry, sealed|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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LXE408 is an oral antileishmanarial compound that selectively targets the kinetoplastid proteosome vs. the mammalian proteosome.
Zetomipzomib (KZR-616) is the first immunoproteasome inhibitor that selectively targets the immunoproteasome subunits LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7). Zetomipzomib has potential for use in a variety of autoimmune diseases.
PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).
|Ixazomib Citrate (MLN9708)
Ixazomib Citrate (MLN9708) immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3.
Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively.
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