Chromatine/Épigénétique

<p>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.</p>

<p>Antidiabetic agent 7 (Compound 5m) functions as a potent hyperglycemia inhibitor. It effectively stimulates GLUT4 translocation in skeletal muscle cells by activating the AMPK-dependent pathway. Additionally, this compound is capable of reducing blood glucose levels and exhibits favorable pharmacokinetic properties. Antidiabetic agent 7 is suitable for research related to antihyperglycemic treatments.</p>

<p>NCT-TFP is PARP probe used to identifying Poly(ADP-ribose) polymerases (PARP) inhibitors[1].</p>

<p>MS479 is a BRD4 PROTAC degrader that binds with high affinity to BRD4-BD2 and GLP (BRD4-BD2: Kd = 200 nM; GLP: Kd = 306 nM). It effectively reduces the protein levels of BRD4 short isoforms. By directly binding to its substrate GLP, MS479 recruits the E3 ligase SPOP as a bridging protein. Additionally, MS479 can be utilized to inhibit the proliferation of colorectal cancer cells.</p>

<p>SJ988497: PROTAC JAK2 degrader, inhibits CRLF2r cell growth, degrades GSPT1, combines Ruxolitinib, linker, Pomalidomide; researched for ALL.</p>

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

<p>HD-TAC7 is a PROTAC HDAC degrader; IC50s: HDAC1 (3.6μM), HDAC2 (4.2μM), HDAC3 (1.1μM); reduces NF-κB p65; researched for asthma, COPD.</p>

<p>Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a PROTAC-based compound designed to degrade CBP and p300, acting as a functional antagonist (WO2020173440).</p>

<p>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%.</p>

<p>SIRT1-IN-1 is a selective inhibitor of SIRT1 with an IC50 of 205 nM.Cost-effective and quality-assured.</p>

<p>EPZ-025654 is an effective and selective inhibitor of arginine methyltransferase CARM1.</p>

<p>PROTACHDAC6 degrader 3 (Compound 4) is a selective inhibitor and degrader of HDAC6, with an IC50 of 686 nM and a DC50 of 171 nM. It enhances the acetylation of α-tubulin. [Pink: ligand for target protein; Blue: ligand for E3ligaseVHL.]</p>

<p>VinSpinIn is a probe for the Spin family proteins.</p>

<p>SIRT5 inhibitor 9 (compound 14) is a moderately selective and substrate-competitive SIRT5 inhibitor with IC50=4.07 μM and has potential anticancer effects.</p>

<p>FHD-609 inhibits and degrades BRD9, aims at ncBAF, aids in diverse cancer research, and may help treat ACC with Telomelysin/INO5401.</p>

<p>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.</p>

<p>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.</p>

<p>G9a-IN-3 (compound 16g) is a potent G9a inhibitor with an IC50 of 0.002 μM. It is applicable for research in sickle cell disease.</p>

<p>dTAG-7 selectively degrades BRD4 and FKBP12F36V by linking BET bromodomains to E3 ligase CRBN; it's a heterobifunctional degrader.</p>

<p>EPZ028862 is a</p>