Cromatina/Epigenetica

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.

MS645 is an inhibitor of bromodomain-containing protein 4 (BRD4) with a Ki of 18.4 nM for BRD4-BD1/BD2.

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%.

PARP1-IN-38 (compound ent-6_P) is a potent PARP1 inhibitor with an IC50 value of 10 μM. It exhibits selective cytotoxic activity in BRCA-mutant cancer cells.

MAK683 hydrochloride is an inhibitor of embryonic ectoderm development (EED), with IC50 values of 59, 26nM measured in EED Alphascreen, ELISA.Cost-effective and quality-assured.

dBAZ2 is a pioneering PROTAC degrader targeting BAZ2A and BAZ2B, with DC50 values of 180 nM for BAZ2A and 250 nM for BAZ2B.

TDI-012804 is a TNKS2 inhibitor that selectively inhibits endogenous TNKS2 protein within cells. It enhances the expression of AXIN1 protein in Tnks1 heterozygous (Tnks1HET) and knockout (Tnks1KO) cells. TDI-012804 suppresses the proliferation of ApcQ1405X/Tnks1KO organoids with an EC50 of 59.1 nM and exhibits selective toxicity towards Tnks1KO AKP-G12D and AKP-G13D organoids.

Novel inhibitor for PKMζ, halts synaptic potentiation and reverses LTP with IC50 of 1-2.5 μM, erasing spatial memory.

NUCC-0226272, a potent PROTAC, induces the degradation of EZH2 and exhibits anti-proliferative effects. It holds promise for application in cancer research [1].

CBB1007 trihydrochloride is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).

Anemonin, a furanone dimer from Buttercups, may help manage melanocytes and osteoarthritis.

PROTAC EED degrader-1 is a PROTAC targeting EED (pKD = 9.02), is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.17.

2-PADQZ hydrochloride shows antiviral activity and targets influenza A virus RNA promoter.

(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

RJW100 is a potent LRH-1 & SF-1 agonist with pEC50 of 6.6 & 7.5, also activates miR-200c promoter.

Ep300/CREBBP-IN-2: Potent, oral Ep300 & CREBBP inhibitor; IC50s: 0.052μM & 0.148μM; 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.

PRMT3-IN-4 (intermediate 15) is an inhibitor of Protein arginine methyltransferase 3 (PRMT3) and serves as the active control for SGC707. It can be utilized in the synthesis of PROTACs targeting PRMT3 and is applicable in research related to leukemia.

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