diffuse

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.

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

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

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].

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).

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.

BF-168 is a candidate probe for PET and specifically recognizes both neuritic and diffuse plaques (Ki: 6.4 nM for Aβ1-42).

IRAK4-IN-6 is a selective and orally efficacious inhibitor of IRAK4, demonstrating an IC50 value of 4 nM. This compound specifically targets MyD88 L265P mutant diffuse large B-cell lymphoma [1].

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).

Dihydroxyacetone phosphate hemimagnesium salt hydrate is also known as dihydroxyacetone phosphate or 3-hydroxy-2-oxopropyl phosphate. Dihydroxyacetone phosphate hemimagnesium salt hydrate is found in all organisms from bacteria to humans. In humans, Dihydroxyacetone phosphate hemimagnesium salt hydrate is involved in many enzymatic reactions. Dihydroxyacetone phosphate hemimagnesium salt hydrate has been studied for the treatment of lymphoma, large cell lymphoma, and diffuse lymphoma.

LDN-214117 is a potent and selective ALK2 inhibitor.

Compound BPP (HDGFRP2 PSIP1-IN-1) is a dual inhibitor targeting the PWWP domains of Hepatoma-derived Growth Factor Related Protein 2 (HDGFRP2) and its homologue PSIP1. This compound effectively hinders the occurrence and progression of Diffuse Intrinsic Pontine Glioma (DIPG). It demonstrates binding affinity with a Kd value of 7 μM for HDGFRP2, indicative of its efficient ligand efficacy at 0.47. Additionally, Compound BPP exhibits a Kd value of 27 μM when binding to the PSIP1 PWWP domain, and a Kd value of 14 μM against HDGFRP3, confirming its potency as an inhibitor within the HDGFRP2 PWWP subfamily.

Compound WK692 (compund WK692) is a BCL6 inhibitor that effectively suppresses the growth of diffuse large B-cell lymphoma cells without toxic side effects and acts synergistically with inhibitors of EZH2 and PRMT5.

FAK-IN-21 (compound 9) is a FAK inhibitor with an IC50 value of 37.52 nM. It inhibits cell growth and the phosphorylation of FAK, making it useful for research into diffuse gastric cancer.

Noradrenaline tartrate is an effective adrenergic receptor agonist that activates α1, α2, and β1 receptors. It is a precursor of epinephrine and serves as the principal neurotransmitter of most postganglionic sympathetic fibers and the diffuse projection system in the brain originating from the locus coeruleus, and can be used to establish cardiomyopathy models.

HDACs EZH2-IN-1 (Compound 22a) is a dual inhibitor of HDACs and EZH2, exhibiting potent inhibitory activity, with EZH2 Y641N being suppressed by 98% at 50 nM. It selectively targets HDAC1 and HDAC6, with IC50 values of 0.23 μM and 0.07 μM, respectively. HDACs EZH2-IN-1 effectively inhibits the proliferation of diffuse large B-cell lymphoma cells harboring EZH2 mutations and various acute myeloid leukemia cells. Additionally, this compound has the capability to induce cellular differentiation and apoptosis (Apoptosis).

M4K2308, a selective ALK2 ether-linked inhibitor, demonstrates an IC50 of 2 nM and exhibits greater specificity for ALK2 over ALK5, with an IC50 of 224 nM for ALK5. This compound holds potential for research into Diffuse Intrinsic Pontine Glioma (DIPG).

BTK-IN-41 (Compound 47) is a BTK inhibitor with an IC50 of 5.4 nM. It inhibits diffuse large B-cell lymphoma cells TDM-8 with an IC50 of 13.8 nM.

M4K2009 is a selective and brain-penetrant ALK2 inhibitor (IC50 = 13 nM) effective against both wild-type (WT) and mutant ALK2 (G328V, R206H, and R258G), used for the treatment of diffuse intrinsic pontine glioma (DIPG).

ASTX295 is a selective mouse double minute 2 (MDM2) antagonist with an IC50 value of less than 1 nM. It specifically inhibits the interaction between MDM2 and p53, reactivating wild-type (WT) TP53, which subsequently induces the expression of related transcriptional targets, leading to cell death and cell cycle arrest. ASTX295 holds potential for research in lymphoid malignancies such as diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), and T-cell lymphoma.

(S,R,S)-AHPC-Boc derivative 1 (Compound 80-9; VH032-Boc derivative 1) is a selective proteasomal degrader targeting MALT1, which recruits the E3 ubiquitin ligase CRBN to form a ternary complex with MALT1. This interaction leads to the ubiquitination and subsequent proteasomal degradation of MALT1. By disrupting the CBM complex, (S,R,S)-AHPC-Boc derivative 1 inhibits the NF-κB signaling pathway and shows potential in inducing apoptosis in ABC-DLBCL cells. It holds promise for research into MALT1-dependent cancers, such as diffuse large B-cell lymphoma (DLBCL).

MNN-02-155 is a bivalent molecular glue that can simultaneously interact with both p300/CBP and BCL6. It effectively induces the activation of BCL6-targeted reporter genes and promotes cell death. This compound is used in the research of diffuse large B-cell lymphoma (DLBCL).

TCIP3 is a bivalent molecular glue (molecular glue) that can simultaneously bind to both p300/CBP and BCL6. It redirects p300 and CBP to activate programmed cell death genes, which are typically repressed by the oncogenic driver BCL6. TCIP3 is useful for studying diffuse large B-cell lymphoma (DLBCL) and is not toxic to untransformed tonsil lymphocytes or fibroblasts.

LD2 is a protein arginine methyltransferase 9 (PRMT9; IC50 = 0.9 µM) inhibitor. It can reduce the proliferation ability of Rec-1 and Raji lymphoblast cells, UPN1 mantle cell lymphoma, BL-41 Burkitt lymphoma, and OCI-Ly3 diffuse large B-cell lymphoma (DLBCL) cells (IC50s = 2.5-5 µM). LD2 (2.5 µM) can induce G2/M phase cell cycle arrest in THP-1 acute myeloid leukemia (AML) cells and reduce the phosphorylation levels of checkpoint kinases 1 (Chk1) and Chk2 in their cells.