Chromatin/Epigenetics

Blocks HIF-1α/β dimerization, not HIF-2α; suppresses VEGF, CAIX in cancer cells; antiangiogenic in HUVECs (IC50 = 1.3 μM).

Go6976 is a PKC inhibitor, widely used in research to probe PKC functions in health and disease.

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.

Sirtuin modulator 5 activates SIRT1 (<50 μM DC50), may extend cell lifespan, and could aid in researching various age/stress-related diseases.

ZMF-23, a PAK1/HDAC6 dual inhibitor, suppresses PAK1 and HDAC6-mediated aerobic glycolysis and cellular migration while inducing TNF-α-regulated necroptosis and

UNC6864, an ethylisopropyllysine-containing ligand, exhibits binding affinity to wild-type CBX5, demonstrating a dissociation constant (K D) of 3.3 μM.

PROTAC BET Degrader-10 targets and degrades BRD4 with a DC50 of 49 nM, using Cereblon ligands.

HDAC6-IN-23 (compound 9), an orally active inhibitor of HDAC6 [1], displays selective enzymatic inhibition.

Menin–KMT2A-IN-1 (Compound 20) is an inhibitor of menin–KMT2A, binding to menin with an IC50 of 8 nM, and disrupting the interaction between menin and lysine methyltransferase 2A (KMT2A). It inhibits hERG channels with an IC50 of 65 μM and suppresses MV4-11 cells with an IC50 of 74 nM. Furthermore, Menin–KMT2A-IN-1 exhibits favorable pharmacokinetic properties in CD-1 mice, with an oral bioavailability of 74%.

SJ1008030 (compound 8) formic is a selective JAK2 degrader within the PROTAC class, demonstrating efficacy in inhibiting MHH-CALL-4 leukemia cell growth with an

JPS016: benzamide VHL E3-ligase PROTAC, degrades HDAC1/2, triggers apoptosis in HCT116 cells.

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.

Kiss2 peptide acetate is the acetate form of Kiss2 peptide, serving as a positive regulator of reproduction. It binds to its homologous receptor Kiss2R (GPR54) in COS-7 cells, activating the PKA and PKC signaling pathways through Gas and Gaq proteins. This activation enhances the activity of both cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc).

PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, demonstrating dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5

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%.

M 1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression.

EZH2-IN-5, potent EZH2 inhibitor; IC50: 1.52 nM (wild-type), 4.07 nM (Tyr641 mutant).

Synthetic peptide analog of bovine myelin basic protein (MBP). Non-competitive inhibitor of PKC (IC50 = 28 - 62 mM).

SARS-CoV-2-IN-87 (compound 138968421) is an effective inhibitor of the SARS-CoV-2 methyltransferases (nsp14 and nsp16).

dBAZ2B is a BAZ2B PROTAC degrader with a DC50 value of 19 nM. (Pink: BAZ2A/B ligand; Black: linker; Blue: CRBN Ligand)