dlbcl

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

TCIP 1 is a small molecule in the category of transcriptional/epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].

Cladribine (2CdA), an adenosine deaminase inhibitor, is utilized in the treatment of lymphoproliferative diseases.

BTM-3566 activates the ISR through the mitochondrial protease OMA1.BTM-3566 induces apoptosis in cancer cells. BTM-3566 overactivates the mitochondrial ISR to study DLBCL.

NBI-961, a potent NEK2 inhibitor, suppresses proteasomal degradation and effectively induces G2/mitosis arrest and apoptosis within diffuse large B cell lymphoma (DLBCL) cells [1].

BCL6 PROTAC 1 is a selective B-cell lymphoma 6 (BCL6) proteolysis targeting chimera (PROTAC) that inhibits the BCL6 cell reporter with an IC50 value of 8.8 µM and significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines, making it valuable for tumor-related research [1].

Anzurstobart (CC-95251; BMS-986351), a fully human monoclonal anti-SIRPα antibody with high affinity, inhibits CD47-SIRPα interaction. It potentiates macrophage-mediated phagocytosis of DLBCL cell lines in co-culture assays with Rituximab and shows promise in solid and hematologic malignancy research [1].

Loncastuximab (RB4v1.2), an anti-CD19 monoclonal antibody, exhibits antitumor properties and holds potential for treating non-Hodgkin's lymphoma (NHL), specifically diffuse large B-cell lymphoma (DLBCL) [1] [2].

ARV-393 is a BCL6 PROTAC degrader with DC50 and GI50 values of <1 nM in both DLBCL and BL cell lines. ARV-393 inhibits tumor volume in multiple tumor xenograft models.

KTX-582 is a potent IRAK4 degrader, exhibiting DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. It efficiently induces apoptosis in MYD88 MT DLBCL and has demonstrated effectiveness in inducing in vivo tumor regressions in a lymphoma model [1] [2] [3].

AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Which Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL).

DM-01 is a potent and selective inhibitor of EZH2. DM-01 can be used to study diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL) and SNF5/INI-1/SMARCB1 gene-associated solid tumours.

Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM). Voruciclib represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma. Voruciclib effectively blocks CDK9, the transcriptional regulator of MCL-1.

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].

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

Avadomide (CC 122) is an orally available pleiotropic pathway modulator with potential antineoplastic activity.

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

Tazemetostat de(methyl morpholine)-COOH (compound 7), a PROTAC ligand for EZH2, facilitates the synthesis of PROTACs that target this enzyme. These EZH2 degraders exhibit potent inhibition of cell viability in diffuse large B-cell lymphoma (DLBCL) and other lymphoma subtypes [1].

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

IRAK4-IN-17 (Compound 5) is a highly potent inhibitor of IRAK4, exhibiting an impressive IC50 value of 1.3 nM [1]. This compound is particularly valuable for research focused on large B-cell lymphoma (DLBCL) [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.

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.

Urelumab(BMS-66513) is a humanized IgG4 monoclonal antibody, often used as a CD137 agonist.Urelumab has potential antitumor activity, potentiating tumor cell killing by T-cells and natural killer cells, and enhancing the cytotoxicity of Rituximab.Urelumab has been used in the study of solid tumor-related diseases such as diffuse large B-cell lymphoma (DLBCL) and follicular lymphoma (FL). Urelumab can be used to study diseases associated with solid tumors such as diffuse large B-cell lymphoma (DLBCL) and follicular lymphoma (FL).

Avadomide is an orally available pleiotropic pathway modulator with potential antineoplastic activity. CC-122 mimics an interferon response and has antitumor activity in DLBCL CC-122 binds Cereblon (CRBN) and promotes degradation of Ikaros and Aiolos in d

IRAK4-IN-27 (Compound 22) is a potent and selective IRAK4 inhibitor, demonstrating an IC50 of 8.7 nM. It effectively suppresses cell growth and induces apoptosis in the MYD88 L265P diffuse large B-cell lymphoma (DLBCL) cell line, positioning it as a valuable agent for DLBCL research [1].

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