dlbcl

Imidazole ketone erastin (IKE) is an ferroptosis inducer with inhibitory effects on system Xc-cystine glutamate transporter proteins. Imidazole ketone erastin has antitumor activity and induces glutathione depletion and lipid peroxidation.

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.

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.

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

ARV-393 is a PROTAC degrader targeting BCL6 with the advantage of being highly potent and orally available.ARV-393 recruits BCL6 and E3 ligase cerebellum to rapidly degrade BCL6 through the cell's natural ubiquitin proteasome system for the treatment of diffuse large b-cell lymphoma (DLBCL) and non-Hodgkin's lymphoma (NHL).

Emavusertib Tosylate (also known as CA-4948) is a potent inhibitor of IRAK4 FLT3 with demonstrated antitumor activity. In cell lines such as ABC DLBCL and AML, CA-4948 exhibits strong cellular efficacy. Among 329 evaluated kinases, it shows medium to high selectivity. The compound has excellent oral bioavailability and favorable pharmacokinetic properties in ADME and PK profiles. In preclinical models involving mice, rats, and dogs, CA-4948 demonstrated good oral bioavailability and displayed over 90% tumor growth inhibition in relevant tumor models, correlating well with in vivo pharmacodynamic regulation.

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.

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

Emavusertib Phosphate (also known as CA-4948) is a potent inhibitor of IRAK4 and FLT3, exhibiting antitumor activity. In ABC DLBCL and AML cell lines, it demonstrates significant cellular efficacy. Furthermore, CA-4948 shows moderate to high selectivity across a panel of 329 kinases and possesses favorable ADME and PK profiles, including good oral bioavailability in mice, rats, and dogs. It achieves over 90% tumor growth inhibition in relevant tumor models and correlates excellently with in vivo PD modulation.

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].

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.

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

BHA536 is an orally effective inhibitor of PKCα β and the NF-kB signaling pathway. This compound inhibits the proliferation of ABC DLBCL cells harboring CD79 mutations by causing cell cycle arrest in the G1 phase and induces apoptosis in TMD8 cells. Additionally, BHA536 exhibits antitumor activity in mice.

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

Emavusertib Maleate (also known as CA-4948) is a potent inhibitor of IRAK4 FLT3, demonstrating antitumor activity. In ABC DLBCL and AML cell lines, CA-4948 exhibited strong cellular activity. It showed moderate to high selectivity in a test against 329 kinases and demonstrated good oral bioavailability in ADME and PK profiles, with effective absorption in mice, rats, and dogs. In relevant tumor models, CA-4948 achieved over 90% tumor growth inhibition and showed excellent correlation with in vivo PD modulation.

Emavusertib Mesylate (also known as CA-4948) is a potent inhibitor of IRAK4 and FLT3, demonstrating antitumor activity. In cell lines of ABC DLBCL and AML, CA-4948 shows significant cellular activity. Moreover, it exhibits moderate to high selectivity in screening assays of 329 kinases and has impressive pharmacokinetic and pharmacodynamic profiles (ADME and PK), with good oral bioavailability in mice, rats, and dogs. In pertinent tumor models, CA-4948 achieves over 90% tumor growth inhibition and shows excellent correlation with in vivo PD modulation.

WK500B is a BCL6 inhibitor that binds to BCL6 within cells, obstructing the BCL6 repression complex and reactivating target genes of BCL6, which leads to the death of DLBCL cells and induces apoptosis and cell cycle arrest. In animal models, WK500B inhibits the formation of germinal centers (GC) and the growth of DLBCL tumors without toxic side effects. Moreover, WK500B demonstrates strong efficacy and favorable pharmacokinetic properties, indicating significant development potential.

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

PI3Kδ BET-IN-1 (compound 10b) exhibits excellent and balanced activity against PI3Kδ (IC50= 112 nM) and BRD4-BD1 (IC50= 19 nM), while also demonstrating strong antiproliferative effects in DLBCL cells.

SJ-106C, a SIRT inhibitor, exhibits IC50 values of 0.59, 0.12, and 0.49 μM against SIRT1 2 3, respectively. This compound specifically targets mitochondria and inhibits the growth of DLBCL tumors.

SGR-1505, an orally active MALT1 allosteric inhibitor, reduces MALT1 enzymatic activity and demonstrates anti-proliferative effects in both BTK inhibitor (BTKi)-sensitive and BTKi-resistant activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines. SGR-1505 is applicable for B-cell lymphoma research [1].

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