Cromatina/Epigenetica

Flindersine is a useful organic compound for research related to life sciences. The catalog number is T124718 and the CAS number is 523-64-8.

METTL16-IN-1 is a potent inhibitor of METTL16, with an IC50 value of 1.7 μM and a Kd value of 1.35 μM. It effectively suppresses the binding of U6 snRNA deletion to the METTL16 MTD, with an IC50 value of 2.5 μM. METTL16-IN-1 also exhibits antitumor activity.

EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).

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.

MAT2A-IN-14 (compound H3) is a MAT2A inhibitor that generates reactive oxygen species (ROS) following ultrasound treatment, leading to the specific degradation of MAT2A in cells through rapid oxidation reactions. When combined with ultrasound, MAT2A-IN-14 induces an 87% reduction of MAT2A in human colon cancer cells.

4-PivO-NMT chloride is an indole derivative-based regulator of the AMPK signaling pathway. It modulates neurogenesis or neurite outgrowth by influencing AMPK activity and holds potential for research in neurological disorders, pain, and inflammation.

PRMT5-IN-34 (Compound C) is an inhibitor of MTA-cooperative protein arginine methyltransferase 5 (PRMT5/MAT).

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%.

dAURK-4, a derivative of Alisertib, functions as a potent and selective degrader of AURKA (Aurora A), exhibiting anticancer properties [1].

HDAC6-IN-42 (compound 2b) is an HDAC6 inhibitor with an IC50 of 0.009 μM, demonstrating significant anti-leukemia activity and synergistic effects with Decitabine, indicating its potential use in the research of Acute Myeloid Leukemia (AML).

Ethyl 2-amino-4-methyl-5-thiophene carboxylate is a SETD7 inhibitor (IC50=4.59μM) with anticancer properties.

PROTAC BRD9 binder moiety 5 selectively binds BRD9 with IC50 4.20μM, used in PROTAC synthesis, shows cancer cell antiproliferative activity.

Eldocasiran, a micro-RNA-193a-3p analogue, exhibits anticancer properties. It is utilized in cancer research [1].

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%.

CEM114 is a potent chemical compound known as a chemical epigenetic modifier (CEM).

PRO-HD2 is a selective, PROTAC-based degrader of HDAC6 [1].

(R)-SKBG-1 is an inhibitor of the RNA-binding protein NONO, effectively downregulating androgen receptor expression by targeting both AR-FL mRNA and AR-V7 mRNA