Chromatine/Épigénétique

<p>Biotin-JQ1 is a bromodomain BRD4 binder; inhibits MM1.S cell growth with EC50 of 0.4μM.</p>

<p>(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</p>

<p>ML234 is a dual inhibitor targeting EZH2/LSD1, with IC50 values of 0.09 and 0.12 μM, respectively. It demonstrates strong antiproliferative effects on prostate cancer cell lines LNCAP, PC3, and 22RV1. Additionally, ML234 inhibits tumor growth in a 22RV1 xenograft mouse model, showing potential as a research agent in prostate cancer therapeutics.</p>

<p>JAK1/STAT3-IN-1 (compound 4f) functions as an anti-atopic dermatitis (AD) agent by inhibiting the JAK1/STAT3 signaling pathway. It has an IC50 value of 2.17 μM for inhibiting NO production. Additionally, JAK1/STAT3-IN-1 improves skin conditions in AD-like mice by reducing inflammatory infiltration, suppressing the expression of p-JAK1/JAK1 and p-STAT3/STAT3, and alleviating the hyperimmune response induced by MC903 (Calcipotriol).</p>

<p>QA-68 is a potent BRD9 degrader, inhibits cell growth, and has anti-leukemic properties.</p>

<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>SGC3027 is an inhibitor of histone methyltransferase,also is a first potent, selective and cell active chemical probe for PRMT7.</p>

<p>HDAC6ligand-3 serves as a ligand for HDAC6 and can be utilized as a target protein ligand in the synthesis of [PROTAC] HDAC6 degrader4.</p>

<p>Malantide TFA: synthetic dodecapeptide, PKA-specific with Km 15 μM, &gt;90% PKI blockage, also PKC substrate, Km 16 μM.</p>

<p>Delcasertib acetate is a selective δ protein kinase C (δPKC) inhibitor for the study of acute myocardial infarction and pain.</p>

<p>GNE-064: Oral SMARCA4/2, PBRM1 inhibitor; IC50 (SMARCA4)=0.035µM, EC50 (SMARCA2)=0.1µM; High solubility; Research probe.</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>EPZ028862 is a</p>

<p>SP-96: Aurora B inhibitor, IC50=0.316 nM, selectively hinders MDA-MD-468 growth, GI50=107 nM, for triple-negative breast cancer research.</p>

<p>Cath-L-dBET1 is a PROTAC degrader targeting BRD4. It has an IC50 value of 2.8 μM in MDA-MB-231 cells. Activated by cathepsin L (Cath-L), Cath-L-dBET1 recruits E3 ubiquitin ligase to degrade BRD4 via the ubiquitin-proteasome system. Hyp-dBET1 is applicable for antitumor research.</p>

<p>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.</p>

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

<p>Pan-BET/BD2-IN-1 (compound 6b) is a selective BET protein inhibitor with BRDT-1Ki of 1.05 μM and BRD4-1Ki of 0.68 μM. It effectively inhibits the growth of MM.1S cancer cells with an IC50 value of 2.6 μM.</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>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>(rel)-Tranylcypromine D5 hydrochloride is a deuterium labeled (rel)-Tranylcypromine hydrochloride.</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>SIRT5 inhibitor 8 (compound 10) is a moderately selective and substrate-competitive SIRT5 inhibitor with IC50=5.38 μM, with potential anticancer effects.</p>

<p>HDAC8-IN-10 (compound 15) serves as a potent inhibitor of HDAC8, exhibiting an IC50 value of 7.6 nM. It also acts as a ligand for the HDAC8 target protein, utilized in the synthesis of PROTAC YX862.</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>OARV-771: VHL-based PROTAC targeting BET; DC50: Brd4-6nM, Brd2-1nM, Brd3-4nM; enhanced cell permeability.</p>

<p>BRD4-binding moiety 1 links to cereblon, forming a PROTAC that degrades BRD4 efficiently.</p>

<p>Mz325 serves as a dual inhibitor of both HDAC and Sirt2, exhibiting an IC50 of 9.7 µM against Sirt2, which are implicated in the pathogenesis of cancer and</p>

<p>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%.</p>

<p>Compound 8b, a dual-ligand PROTAC, targets VHL &amp; BRD4, degrades BRD4 in PC3 cells; conjugates with STEAP1/CLL1, DC50: 1.3/18 nM.</p>

<p>Pim-1 kinase inhibitor 11 (10f) is an inhibitor of PIM-1 with an IC50 value of 0.18 μM. It exhibits anticancer activity by inducing apoptosis and causing cell cycle arrest.</p>

<p>Uzansertib (INCB053914) is a potent pan-PIM kinase inhibitor with low IC50s: 0.24, 30, 0.12 nM for PIM1, 2, 3; hinders hematologic tumor growth.</p>

<p>Tert-butyl compound inhibits human EGLN-1; confirmed by spectrometry after 20 mins.</p>

<p>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.</p>

<p>Compound 1769-24-0 is a natural product for research related to life sciences. The catalog number is TPL0186 and the CAS number is 1769-24-0.</p>

<p>R 8605 is a third-generation retinoid.</p>

<p>PROTAC BRM degrader-1 (compound 17) serves as a PROTAC-based degrader targeting both BRM and BRG1, exhibiting DC50 values of 93 pM and 4.9 nM, respectively [1].</p>

<p>TB22 is a non-nucleoside inhibitor of DOT1LR231Q with anticancer activity. It inhibits the malignant phenotype of lung cancer cells harboring the R231Q mutation via the MAPK/ERK signaling pathway, making it useful for lung cancer research.</p>

<p>UNC10142 (Compound 44) is a small-molecule antagonist of CHD1, with a binding IC50 value of 1.7 μM. It induces a dose-dependent reduction in the viability of PTEN-deficient prostate cancer cells.</p>

<p>SW2_152F: Potent CBX2 ChD inhibitor, Kd 80 nM, 24-1000x selective over other CBXs in vitro.</p>

<p>BTR2004 is a selective PROTAC degrader targeting the BET family (BRD2/3/4) proteins. It facilitates the formation of a ternary complex with BRD proteins and KLHL20, leading to ubiquitination and proteasomal degradation via the UPS pathway. BTR2004 shows potential for research in PC3 prostate cancer and MDA-MB-231 breast cancer cell lines.</p>

<p>NF-κB/HIF-1α-IN-1 (compound 9c) effectively inhibits the NF-κB activation pathway and demonstrates selective antifibrotic activity. This compound exhibits no significant cytotoxicity in NCI tumor cell lines. In rat models, NF-κB/HIF-1α-IN-1 successfully ameliorates liver fibrosis, suppresses the expression levels of NF-κB and HIF-1α, and induces Nrf2.</p>

<p>Biguanide can reduce oxidative stress in rats with hyperglycemia.</p>

<p>BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.</p>

<p>SJ1008030, a JAK2 PROTAC, degrades JAK2; EC50: 5.4 nM, IC50: 32.09 nM in MHH-CALL-4 cells for leukemia research.</p>

<p>HSP90/LSD1-IN-1 (compound 6) is a dual inhibitor of HSP90 and LSD1. This compound effectively inhibits the proliferation of prostate cancer cell lines PC-3 and DU145, with GI50 values of 0.24 μM and 0.30 μM, respectively.</p>