Chromatin/Epigenetics

BAY-155 is a powerful and selective menin-MLL inhibitor, exhibiting an IC 50 of 8 nM. It significantly down-regulates MEIS1 gene expression while up-regulating CD11b and MNDA genes. BAY-155 also demonstrates anti-proliferative effects in AML/ALL (acute myeloid/lymphoblastic leukemia) models [1].

PROTAC BRD4 Degrader-7, from patent WO2020055976A1, has IC50 of 15.5 nM (BD1) & 12.3 nM (BD2).

dBRD9 is a PROTAC.

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

PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.

HDAC-IN-68 (hydrochloride) (Compound 29) is an HDACs inhibitor with an IC50 value of 0.04 μM and induces microtubule fragmentation by activating katanin, a microtubule-severing protein. It is applicable in cancer research.

α-Hydroxyglutaric Acid is a natural product for research related to life sciences. The catalog number is T36624 and the CAS number is 2889-31-8.

CDD-1102 HCl is a novel BRDT-BD4 / BRD2-BD1302 selective inhibitor that shows non-hormonal contraceptive potential in ex vivo experiments.

ZXH-3-26 is a PROTAC composed of a Cereblon ligand, an E3 ubiquitin ligase, and a BRD4 ligand that can be used to study cancer.

CBPD-409 is an orally active CBP/p300 degrader with a DC50 of 0.2–0.4 nM. It exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP, and 22Rv1, with an IC50 of 1.2–2.0 nM. Additionally, CBPD-409 shows antitumor activity.

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

PRMT5-IN-12 shows remarkable inhibitory activity on PRMT5 .

PI3Kα/HDAC6-IN-1 (compound 21j) is a dual inhibitor of PI3Kα and HDAC6, exhibiting IC50 values of 2.9 nM and 26 nM, respectively.

Protein Kinase C (19-31), a PKC inhibitor derived from PKCa, has a serine at position 25 and tests PKC activity.

TO-1187 TFA is a selective HDAC6 PROTAC degrader with a DC50 of 5.81 nM. It facilitates the ubiquitination and degradation of HDAC6 and is applicable to research in hematologic malignancies and solid tumors.

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.

HIV-1 protease-IN-10 (Compound 2), exhibiting HIV-1 latency reversing activity (IC50: 0.22 μM), selectively binds to the PKCδ C1b domain (IC50: 0.69 μM) and

PKCβII Peptide Inhibitor I, a specific PKCβII inhibitor, exhibits cardioprotective properties in a rat cardiac ischemia/reperfusion injury model and mitigates

PRMT5-IN-14 is a PRMT5 inhibitor to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.

JPS014: A potent benzamide-based VHL E3-ligase PROTAC that degrades HDAC1/2, altering gene expression and inducing apoptosis in HCT116 cells.

HAT-SIL-TG-1&AT: a hypoxia-activated JAK inhibitor that curbs HEL cell growth & STAT3/5 phosphorylation in tumors.

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.

PROTACBRD4 Degrader-31 is a BRD4 PROTAC degrader with DC50 values of 164 nM at 4 hours and 80 nM at 24 hours. It effectively degrades BRD4 within cells and exhibits long-lasting degradation kinetics.

UNC6852 contains an EED ligand (IC50 = 247 nM) and a von Hippel-Lindau ligand and is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC.

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%.

GSK232 is a highly selective and cellularly penetrant inhibitor of CECR2 with outstanding physicochemical properties.

BRCA1-IN-1 is a novel small-molecule-like inhibitor of BRCA1 (IC50: 0.53 μM; Ki: 0.71 μM).

Echinomycin (Quinomycin A) is a quinoxaline antibiotic and a DNA-intercalating peptide that inhibits hypoxia-inducible factor-1 (HIF-1) DNA binding activity.

BB-Cl-Amidine (TFA) is an inhibitor of peptidylarginine deiminase (PAD).

Axltide mimics mouse Insulin receptor substrate 1, amino acids 979-989 with sequence KKSRGDYMTMQIG.

Curcuphenol in concentrations in the range of 29-116 μg/ml inhibited cell proliferation and DNA replication and induced cell death in a dose-dependent manner.

Retreversine serves as an inactive control counterpart to Reversine, a pioneering class of ATP-competitive Aurora kinase inhibitor.

7-Hydroxyneolamellarin A, from Dendrilla nigra, inhibits HIF-1α and VEGF in cancer research.

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).

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.

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%.

CBP/p300-IN-14, patent WO2021213521A1's compound 27, inhibits CBP/EP300 with 3.3 nM IC50.

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

PROTACBRD4 Degrader-34 is a selective BRD4 PROTAC degrader (pDC50= 8.4) that induces VHL-mediated BD2 degradation and is applicable for cancer research.

GSK3735967: DNMT1 inhibitor, IC50 40 nM, dicyanopyridine core, binds hemimethylated CpG, interacts with H4K20me3.

CAM2602 is an inhibitor of Aurora A-TPX2 interaction, demonstrating a binding affinity of 19 nM with Aurora A. This compound has been shown to inhibit the growth of pancreatic cancer cells. In solid tumor xenograft models, CAM2602 increases the proportion of PH3-positive cells while decreasing the ratio of P-Thr288Aurora A-positive cells, ultimately inhibiting tumor growth.

PROTAC BRD4 Degrader-13 targets VHL and BRD4, degrading BRD4 with DC50 of 0.025/6.0 nM in PC3 cells when linked to STEAP1/CLL1 antibodies.

MR44397 is a ligand for WD40 repeat (WDR) 5 and is applicable in cancer research.

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

Dihydrochlamydocinanalog-1 (compound 2) is a Chlamydocin analog that inhibits the deacetylation of histone H4 peptides, with an IC50 of 30 nM.

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology(Kd of 4 nM for Brd4BD2)

PROTACBRD4 Degrader-33 is an enzyme-activated, click-responsive BRD4 PROTAC degrader designed with effective tumor microenvironment responsiveness. This compound exhibits exceptional penetration into tumor tissues and effectively inhibits PD-L1 protein expression. In the 4T1 tumor mouse model, PROTACBRD4 Degrader-33 demonstrates potent antitumor immunomodulatory activity.