M3258_product_DataBase

Bioactivity

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[1][2].

Invitro

M3258 inhibits human LMP7 with a mean IC50 of 4.1 nM. 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[2].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)[2]. Cell Viability Assay[2] Cell Line:

Name

M3258

CAS

2285330-15-4

Formula

C17H20BNO5

Molar Mass

329.16

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

PeptideDB

M3258

CAS: 2285330-15-4 F: C17H20BNO5 W: 329.16