Chromatin/Epigenetics

MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. This compound delivers Verteporfin to CD206+ tumor-associated macrophages (TAM), thereby inhibiting the YAP/TAZ signaling pathway. It facilitates YAP exclusion from the nucleus, induces TAM polarization toward an anti-tumor phenotype, enhances phagocytosis and antigen presentation, and promotes T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models.

Mz325 serves as a dual inhibitor of both HDAC and Sirt2, exhibiting an IC50 of 9.7 µM against Sirt2, which are implicated in the pathogenesis of cancer and

E67-2: Low-toxic, KIAA1718 inhibitor with IC50 of 3.4μM, targets H3K9/H3K4 demethylases.

WDR5ligand 2 is a ligand for WDR5 and can be utilized in the synthesis of PROTAC WDR5degrader 1.

Martinostat is an HDAC inhibitor that can be radiolabeled for quantitative imaging of HDACs within the central nervous system and major peripheral organs.

SIRT-IN-5, a selective inhibitor of SIRT3 with an IC50 of 2.88 μM, facilitates the differentiation of multiple myeloma cells. This differentiation is associated with increased expression of the differentiation antigens CD49e and human immunoglobulin light chains λ and κ.

Aurothiomalate tetramer sodium, a tetrameric form of Aurothiomalate sodium, functions as an anti-arthritis gold agent. It also acts as a potent and selective inhibitor of the oncogenic PKCι signaling pathway.

HIF1-IN-3 (Benzenepropanamide, N-[(8-hydroxy-7-quinolinyl)(4-methoxyphenyl)methyl]-) is an effective inhibitor of HIF-1 (EC50 = 0.9 μM) and can be used in

SAHA inhibits class I/II HDAC; c-SAHA, a fluorescent derivative, excites at 325 nm and emits at 400 nm.

BI01826025 (pArg-JQ1), a BRDT BD1 bromodomain PROTAC degrader, tests ClpC2's effect on ClpC1P1P2 protease.

SMD-3236 is a PRAOTAC degrader targeting SMARCA2, designed using SMARCA ligand and VHL-1 ligand, and exhibits prolonged anti-tumor activity in vivo. SMARCA2 acts as a synthetic lethal target in cancer cells lacking SMARCA4, with SMD-3236 showing 2000-fold selectivity for SMARCA2 over SMARCA4, having a DC50 of less than 1 nM and a Dmax of over 95%. In the human cancer xenograft models deficient in SMARCA4, notably the H838 model, SMD-3236 effectively induces loss of SMARCA2 in tumor tissue while sparing the SMARCA4 protein, thereby inhibiting tumor growth. The compound consists of a target protein ligand (red part) SMI-1074, a PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate, and an E3 ligase ligand (blue part) SMARCA2 ligand-14, forming the E3LigaseLigand-linker Conjugate 159.

Dihydrochlamydocin, an inhibitor of histone deacetylases (HDAC), exhibits potent cytostatic activity against mastocytoma cells.

iRucaparib-AP6: a specific, non-trapping PARP1 degrader; inhibits the enzyme's activity and scaffolding.

PARP/HDAC-IN-1 is a PARP and HDAC inhibitor that inhibits PARP1, PARP2, and HDAC1, and may be used to study pancreatic cancer.

HDAC1-IN-9 (13c) is an HDAC1 inhibitor. It inhibits the HDAC1 enzyme with an IC50 value of 1.07 µM. This compound exhibits the strongest antiproliferative activity against HT-29 (human colon adenocarcinoma cells), with an IC50 of 1.78 μM. In HCT-116 (human colon cancer cells), HDAC1-IN-9 significantly induces apoptosis. Additionally, HDAC1-IN-9 possesses antiangiogenic properties, reducing the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80%.

DW71177 is a BET inhibitor with potent anti-leukemic activity for the study of leukemia.

PAD2-IN-1 is a selective benzimidazole-derived inhibitor with a 95-fold and 79-fold higher affinity for PAD2 over PAD4 and PAD3, respectively.

WQQ-345, a BCAT1 inhibitor, exhibits an IC50 of 10.8 mM. In 67R cells, it reduces α-KG levels and upregulates H3K27me3 expression while downregulating the expression of glycolytic enzymes (PFKP and LDHA), leading to impaired glycolytic activity. Additionally, WQQ-345 demonstrates tumor-suppressive activity in a 67R subcutaneous xenograft model.