abc-dlbcl

Mepazine (Pecazine) is a potent and selective inhibitor of MALT1, inhibiting GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 μM and 0.42 μM, respectively. Mepazine enhances apoptosis and impacts cell viability.

IRAK4-IN-7 (CA-4948) is a selective and potent IRAK4 kinase inhibitor with in vivo activity in a TLR4-induced cytokine release model.

MLT-231, a potent and highly selective allosteric MALT1 inhibitor, has an IC50 of 9 nM and specifically inhibits endogenous BCL10 cleavage with an IC50 of 160 nM. It exhibits antitumor activity in an ABC-DLBCL type xenograft mouse model[1].

iNUB is a NEMO-Ub binding inhibitor. iNUB inhibits TNFα induced NF-κB signaling and has selectively toxic to IKK/NF-κB dependent ABC-DLBCL.

(R)-MLT-985 (compound 11) is a potent MALT1 protease inhibitor (IC50: 3 nM) and has an IC50 value of 20 nM for MALT1-dependent IL-2 in Jurkat cells. Additionally, (R)-MLT-985 inhibits the growth and aberrant CARD11 BCL10 MALT1 complex signaling in ABC-DLBCL cells.

IRAK4-IN-15 is a selective and potent IRAK4 inhibitor (IC50: 0.002 μM) with good human PK prediction and low intrinsic clearance.IRAK4-IN-15 in combination with Acalabrutinib exhibited potent synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL.

IRAK4-IN-14 is a selective, potent, orally active IRAK4 inhibitor (IC50: 0.003 μM) with favorable PK parameters in rats and mice. effect.

Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor, with IC50 values of 0.83 μM for GSTMALT1 full length and 0.42 μM for GSTMALT1 325-760. It enhances apoptosis and affects the viability of ABC-DLBCL cells [1].