Cromatina/Epigenetica
Gli inibitori della cromatina/epigenetica sono composti che modulano la struttura e la funzione della cromatina o interferiscono con le modificazioni epigenetiche, come la metilazione del DNA e la modifica degli istoni. Questi inibitori sono strumenti essenziali per studiare la regolazione dell'espressione genica e il ruolo dell'epigenetica in malattie come il cancro, i disturbi neurologici e le anomalie dello sviluppo. Mirando ai processi epigenetici, questi inibitori possono alterare i modelli di espressione genica e offrire nuove opportunità terapeutiche. Presso CymitQuimica, offriamo un'ampia selezione di inibitori della cromatina/epigenetica di alta qualità per supportare le tue ricerche in biologia molecolare, genetica ed epigenetica.
Sottocategorie di "Cromatina/Epigenetica"
Trovati 2490 prodotti di "Cromatina/Epigenetica"
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EED ligand 1
EED ligand 1: potent PRC2 inhibitor targeting EED subunit.Formula:C19H19FN8OColore e forma:SolidPeso molecolare:394.41MDH1/2-IN-1
CAS:MDH1/2-IN-1 is an MDH1/2 inhibitor with IC50 values of 1.07 nM and 1.06 nM, respectively. It suppresses mitochondrial respiration and the HIF-1α pathway. MDH1/2-IN-1 exhibits significant antitumor potential and offers new avenues for developing drugs targeting cancer metabolism.Formula:C25H33NO4Colore e forma:SolidPeso molecolare:411.534cis-4-Br-2,5-F2-PCPA
cis-4-Br-2,5-F2-PCPA (S1024) blocks LSD1/LSD2 (Ki: 94 nM/8.4 μM), hinders cancer stem cell growth, raises H3K4me2 in CCRF-CEM cells.Formula:C9H8BrF2NColore e forma:SolidPeso molecolare:248.07BET-IN-27
CAS:BET-IN-27 (compound 6C) is an orally active BET inhibitor with IC50 values of 3.3 nM (BRD4-BD2), 3.4 nM (BRD4-BD1), 4.1 nM (BRD2-BD1), 20.4 nM (BRD3-BD1), and 42.0 nM (BRDT-BD1). It also exhibits antiproliferative activity.Formula:C21H23N5O3SColore e forma:SolidPeso molecolare:425.5JAK2-IN-11
CAS:JAK2-IN-11 (Example 6) is a JAK2 kinase inhibitor with potent antitumor activity, exhibiting an IC50 of ≤10 nM against JH2 BIND WT/V617F. This compound effectively suppresses tumor growth.Formula:C31H31F3N8O4Colore e forma:SolidPeso molecolare:639.64Basroparib
CAS:Basroparib is an inhibitor of ribose polymerase (PARP) and has shown antitumour effects.Formula:C18H21F2N7O3Colore e forma:SolidPeso molecolare:421.4PARP1-IN-30
CAS:PARP1-IN-30 is a specific and effective PARP1 inhibitor with cytotoxic properties. It precisely inhibits PARP1 in tumor cells lacking breast cancer 1 protein (BRCA1) or BRCA2. PARP1-IN-30 holds potential for use in cancer research.Formula:C14H12ClNO4SColore e forma:SolidPeso molecolare:325.77KSQ-4279 (gentisate)
CAS:KSQ-4279 (gentisate) (Compound Formula I) serves as an effective inhibitor of USP1 and a selective inhibitor of PARP1. This compound shows promise for use in cancer research.Formula:C34H31F3N8O5Colore e forma:SolidPeso molecolare:688.66L-Moses dihydrochloride
L-Moses (L-45) dihydrochloride is the first, potent, selective p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor (Kd: 126 nM).Formula:C21H26Cl2N6Colore e forma:SolidPeso molecolare:433.38RU-0415529
CAS:RU-0415529 is an orally active inhibitor of SARS-CoV-2 non-structural protein 14 (NSP14), with an IC50 of 356 nM. It inhibits viral RNA methylation and replication by stabilizing the cap-binding pocket through SAH binding. Additionally, RU-0415529 exhibits anti-infective activity in mouse models.Formula:C21H29N3O4SColore e forma:SolidPeso molecolare:419.538QCA570
CAS:QCA570 is an effective BET degrader based on PROTAC (IC50: 10 nM for BRD4 BD1 Protein).Formula:C39H33N7O4SPurezza:98%Colore e forma:SolidPeso molecolare:695.79XP5
XP5 is an oral HDAC6 inhibitor, potent against cancer cells, including YCC3/7 (IC50=31 nM to 2.31 μM).Formula:C19H25N3O5SColore e forma:SolidPeso molecolare:407.48PARP14 inhibitor 1
CAS:PARP14 inhibitor1 (compound Q22) is a selective inhibitor of PARP14 with an IC50 of 5.52 nM. It also exhibits anti-inflammatory properties and has a half-life of 182 minutes in mouse liver microsomes. This compound is applicable for atopic dermatitis research.
Formula:C23H27FN4O3Colore e forma:SolidPeso molecolare:426.484CBP/p300-IN-16
CBP/p300-IN-16 (compound 1) is a potent inhibitor of EP300/CBP HAT, acting on HAT EP300 (IC50: 0.61 μM) and LK2 H3K27 (IC50: 2.24 μM).Formula:C26H31N3O4Colore e forma:SolidPeso molecolare:449.54O-Desmethyl Midostaurin
CAS:O-Desmethyl Midostaurin is the active Midostaurin metabolite via cytochrome P450 liver enzyme metabolism.Formula:C34H28N4O4Purezza:98%Colore e forma:SolidPeso molecolare:556.61HDAC6-IN-9
CAS:HDAC6-IN-9 is a γ-secretase modulator that can significantly reduce the level of Aβ42 in mouse brain and can be used to study neurological diseases.Formula:C19H16N2O3Purezza:98.84%Colore e forma:SolidPeso molecolare:320.34JAK3-IN-7
CAS:JAK3-IN-7 is a potent and selective JAK3 inhibitor (IC50<0.01 μM) for the treatment of rejection in organ transplantation, graft-versus-host reaction afterFormula:C17H20N6OPurezza:98.81%Colore e forma:SolidPeso molecolare:324.38Triciferol
CAS:Triciferol is a VDR agonist and HDAC antagonist with 1,25D-like potency, affecting gene targets and tubulin, and shows anti-cancer effects in vitro. IC50=87nM.Formula:C26H39NO4Colore e forma:SolidPeso molecolare:429.591NPC26
CAS:NPC26 is a small molecule that disrupts mitochondrial function and exhibits antitumor activity. It shows significant antiproliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 induces mitochondrial permeability transition pore (mPTP) opening, generates reactive oxygen species (ROS), and triggers cell death. Additionally, NPC26 kills CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway.Formula:C19H23N3O5S2Colore e forma:SolidPeso molecolare:437.533MS8815
CAS:MS8815 is a selective EZH2 PROTAC degrader with IC50 of 8.6 nM, used in triple-negative breast cancer research.Formula:C65H87N9O8SColore e forma:SolidPeso molecolare:1154.51HDAC-IN-27
HDAC-IN-27 is a potent and orally active inhibitor of HDAC Class I (0.43 nM - 3.01 nM for HDAC1-3).Formula:C20H22N4O2Colore e forma:SolidPeso molecolare:350.41HDAC6-IN-13
HDAC6-IN-13: potent, selective HDAC6 inhibitor; oral; IC50=0.019μM; targets HDAC1/2/3; crosses blood-brain barrier; anti-inflammatory.Formula:C23H22N4OColore e forma:SolidPeso molecolare:370.45KDOAM-25 citrate
CAS:KDOAM-25 citrate inhibits KDM5A/B/C/D (IC50: 71, 19, 69, 69 nM); boosts H3K4 methylation, hinders MM1S cell growth. [1]Formula:C21H33N5O9Purezza:98%Colore e forma:SolidPeso molecolare:499.51HIF-1/2α-IN-1
HIF-1/2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α.Formula:C17H16N6O4Colore e forma:SolidPeso molecolare:368.35DCHC
CAS:DCHC is an activator of SIRT1, but it does not induce SIRT1 expression. This compound can be utilized in studies related to mitochondrial damage.Formula:C15H8Cl2O3Colore e forma:SolidPeso molecolare:307.128NMDAR/HDAC-IN-1
Compound 9d is a dual NMDAR and HDAC inhibitor with high NMDAR affinity (Ki=0.59 μM) and inhibits HDAC1-3,6,8; crosses the blood-brain barrier.Formula:C22H28N2O3Colore e forma:SolidPeso molecolare:368.47PARP-1-IN-1
PARP-1-IN-1: Selective, oral PARP-1 inhibitor with 0.96 nM IC50; well-tolerated and effective in single-dose MDA-MB-436 model.Formula:C23H25FN4OColore e forma:SolidPeso molecolare:392.47MAO A/HDAC-IN-1
MAO A/HDAC-IN-1 is an effective monoamine oxidase A (MAO A) and HDAC dual inhibitor, which can be used for glioma research.Formula:C21H24ClN3O3Colore e forma:SolidPeso molecolare:401.89CFT8634
CAS:CFT8634 degrades BRD9, for synovial sarcoma and SMARCB1 tumor research, from patent WO2021178920A1.Formula:C37H45F3N6O5Colore e forma:SolidPeso molecolare:710.79SIRT1-IN-5
CAS:SIRT1-IN-5 (215) is a modulator of NAD-dependent deacetylase SIRT1 with potential applications in cancer and cellular signaling research.Formula:C21H17N3O3SPurezza:99.97%Colore e forma:SolidPeso molecolare:391.44CEE321
CAS:CEE321 is an effective pan-JAK inhibitor with an IC50 of 54 nM. It effectively inhibits biomarkers associated with atopic dermatitis.Formula:C18H16ClN5OColore e forma:SolidPeso molecolare:353.806AMPTX-1
CAS:AMPTX-1 is a molecular glue functioning as a potent, selective, and reversible covalent degrader of BRD9 by recruiting it to the E3 ligase DCAF16.Formula:C42H53N5O4Colore e forma:SolidPeso molecolare:691.901(Rac)-Nanatinostat
CAS:(Rac)-Nanatinostat ((Rac)-CHR-3996, example 44) is a potent HDAC inhibitor with an IC50 of less than 330 nM. It exhibits anticancer properties, effectively inhibiting the growth of HeLa, U937, and HUT cells.Formula:C20H19FN6O2Colore e forma:SolidPeso molecolare:394.402TK-129
TK-129: Oral KDM5B inhibitor, IC50=44 nM, low-toxicity, cardioprotective, aids in heart disease research.Formula:C15H23N5O2Colore e forma:SolidPeso molecolare:305.38NSD2-PWWP1-IN-3
CAS:NSD2-PWWP1-IN-3 (compound 36) is an effective inhibitor of NSD2-PWWP1, with an IC50 value of 8.05 µM. It has potential applications in cancer research.
Formula:C34H39N5O2Colore e forma:SolidPeso molecolare:549.706HIF-1α-IN-5
HIF-1α-IN-5 is an inhibitor of HIF-1α with an IC 50 value of 24 nM in HEK293T cells that also inhibits the activity of MAO-A.Formula:C16H15N3O2Colore e forma:SolidPeso molecolare:281.31iBFAR2
CAS:iBFAR2, an inhibitor of BFAR, restores the CD8+ tumor-resident memory T cell subset against solid tumors. It promotes the binding of JAK2-STAT1 and enhances the phosphorylation of STAT1.
Formula:C19H15F3N2O2Colore e forma:SolidPeso molecolare:360.33JAK-IN-19
JAK-IN-19 inhibits JAK (pIC50: 7.2, 7.7), less so for VEGFR2 (7.0) and Aurora B (5.8).Formula:C26H36FN5O2Colore e forma:SolidPeso molecolare:469.59HDAC6-IN-3
HDAC6-IN-3 (Compound 14) is an oral anti-prostate cancer agent, inhibiting HDACs and MAO-A, with IC50 of 0.02-1.54 μM.Formula:C19H27N3O3Colore e forma:SolidPeso molecolare:345.44MAT2A-IN-24
CAS:MAT2A-IN-24 (Compound 9) is an inhibitor of methionine adenosyltransferase 2a (MAT2a), with an IC50 value of 20 nM for MAT2a inhibition and an antiproliferative IC50 value of 10 nM for HAP1MTAP–/– cells. MAT2A-IN-24 is applicable in the research of tumor diseases associated with MTAP deficiency.Formula:C32H33Cl2N7O2Colore e forma:SolidPeso molecolare:618.556HDAC8-IN-2
HDAC8-IN-2 (5o) inhibits both smHDAC8 and hHDAC8 with IC50s of 0.27 μM, 0.32 μM, kills schistosome larvae, and lowers egg laying.Formula:C21H16N2O5Colore e forma:SolidPeso molecolare:376.36Trichostatin A S-isomer
CAS:Trichostatin A S-isomer, a HDAC 1, 3, 4, 6, 10 inhibitor with IC50 ~20 nM, has wide-ranging epigenetic effects.Formula:C17H22N2O3Purezza:98%Colore e forma:SolidPeso molecolare:302.37TYK2 ligand 2
CAS:TYK2ligand 2 is the TYK2 ligand of PROTACTYD-68. TYD-68 is a highly potent and selective CRBN-recruiting TYK2 PROTAC degrader with a DC50 value of 0.42 nM.Formula:C24H20FN7O4Colore e forma:SolidPeso molecolare:489.458Itareparib
CAS:Itareparib is a PARP inhibitor with demonstrated antitumor activity.Formula:C20H26FN3O2Colore e forma:SolidPeso molecolare:359.438LSD1-IN-22
LSD1-IN-22: potent LSD1 inhibitor, K_i 98 nM, curbs cancer cell growth.Formula:C9H8BrF2NColore e forma:SolidPeso molecolare:248.07Pociredir
CAS:Pociredir (FTX-6058), a potent EED inhibitor (KD=0.163 nM), may help in SCD research.Formula:C22H18FN5O2Colore e forma:SolidPeso molecolare:403.41PRMT5-MTA-IN-3
CAS:PRMT5-MTA-IN-3 (Compound P2A) is an orally active and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It inhibits the proliferation of MTAP-deficient colorectal cancer HCT-116 cell line with an IC50 value of 5 nM. PRMT5-MTA-IN-3 holds potential for research in cancers, particularly in MTAP-deficient tumors such as colorectal cancer, non-small cell lung cancer, and pancreatic cancer.Formula:C19H17F3N6O3Colore e forma:SolidPeso molecolare:434.372LSD1-IN-15
LSD1-IN-15 inhibits LSD1, MAO-A/B with IC50s: 0.149, 0.028, 0.327 μM; arrests LNCaP cancer cell growth, IC50 9.9 μM.Formula:C22H20N2OColore e forma:SolidPeso molecolare:328.41Purinostat
CAS:Purinostat is a selective inhibitor of HDACI/IIb with potential anti-leukemic properties. Its mesylate form, Purinostat mesylate, is effective at inhibiting the survival of Ph+ leukemic cells and CD34+ leukemic cells derived from CML patients. Purinostat mesylate targets HDACI/IIb, impacting several crucial factors for leukemia stem cell (LSC) survival, such as c-Myc, β-Catenin, E2f, Ezh2, Alox5, and mTOR. Additionally, Purinostat mesylate enhances glutamate metabolism in LSCs by increasing GLS1.Formula:C23H26N10O3Colore e forma:SolidPeso molecolare:490.518AMPK activator 16
CAS:AMPK activator16 (compound 6) functions as an AMP-activated protein kinase (AMPK) inhibitor. It interacts effectively with crucial AMPK residues, significantly activating the enzyme. In N2a cells, AMPK activator16 enhances the expression of phosphorylated AMPK (p-AMPK) and its downstream signaling proteins, such as phosphorylated ACC (Acetyl-CoA Carboxylase) and phosphorylated raptor (p-raptor).Formula:C23H20ClNO5SColore e forma:SolidPeso molecolare:457.927
