Product Name :
M3258
Description:
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells.
CAS:
2285330-15-4
Molecular Weight:
329.16
Formula:
C17H20BNO5
Chemical Name:
[(1R)-2-(1-benzofuran-3-yl)-1-[(1S,2R,4R)-7-oxabicyclo[2.2.1]heptan-2-yl]formamidoethyl]boronic acid
Smiles :
OB(O)[C@H](CC1=COC2C=CC=CC1=2)NC(=O)[C@@H]1C[C@H]2CC[C@@H]1O2
InChiKey:
RFQDLTYXNINJON-OYNZBZHQSA-N
InChi :
InChI=1S/C17H20BNO5/c20-17(13-8-11-5-6-15(13)24-11)19-16(18(21)22)7-10-9-23-14-4-2-1-3-12(10)14/h1-4,9,11,13,15-16,21-22H,5-8H2,(H,19,20)/t11-,13-,15+,16+/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.Clobetasol propionate Inhibitor 6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells.|Product information|CAS Number: 2285330-15-4|Molecular Weight: 329.16|Formula: C17H20BNO5|Chemical Name: [(1R)-2-(1-benzofuran-3-yl)-1-[(1S,2R,4R)-7-oxabicyclo[2.2.1]heptan-2-yl]formamidoethyl]boronic acid|Smiles: OB(O)[C@H](CC1=COC2C=CC=CC1=2)NC(=O)[C@@H]1C[C@H]2CC[C@@H]1O2|InChiKey: RFQDLTYXNINJON-OYNZBZHQSA-N|InChi: InChI=1S/C17H20BNO5/c20-17(13-8-11-5-6-15(13)24-11)19-16(18(21)22)7-10-9-23-14-4-2-1-3-12(10)14/h1-4,9,11,13,15-16,21-22H,5-8H2,(H,19,20)/t11-,13-,15+,16+/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 250 mg/mL (759.51 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|M3258 inhibits human LMP7 with a mean IC50 of 4.Varenicline manufacturer 1 nM.PMID:33186087 M3258 displays weak activity against the constitutive proteasome subunit β5 (mean IC50=2519 nM). M3258 potently inhibits LMP7 in the human multiple myeloma cell lines MM.1S and U266B1 and in human, rat, and dog PBMCs with IC50s between 2 and 37 nM. M3258 induces a >four fold accumulation of ubiquitinated proteins with an EC50 of 1980 nM in MM.1S cells. M3258 interferes with immunoproteasome function. M3258 also induces apoptosis assessed by caspase 3/7 activity (EC50=420 nM;>3.5-fold induction) and reduces MM.1S cell viability (IC50=367 nM).|In Vivo:|M3258 (1 mg/kg; 10 mg/kg) shows superior antitumor efficacy in selected multiple myeloma and mantle cell lymphoma xenograft models compared with the approved nonselective proteasome inhibitors bortezomib and ixazomib.|Products are for research use only. Not for human use.|