Search Result
Results for "
H3K4me
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
상품명 |
Target |
연구분야 |
Chemical Structure |
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- HY-100421
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CPI-455
Maximum Cited Publications
13 Publications Verification
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Histone Demethylase
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Cancer
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CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
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- HY-120400
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Histone Demethylase
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Cancer
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KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels .
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- HY-12583
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Histone Methyltransferase
Epigenetic Reader Domain
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Cancer
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A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
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- HY-16705
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BRD4770
5 Publications Verification
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Histone Methyltransferase
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Cancer
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BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 μM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence .
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- HY-100421A
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Histone Demethylase
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Cancer
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CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
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- HY-403538
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Zinc Finger Protein
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Cancer
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iZMYND8-34 is a ZMYND8 inhibitor with an IC50 of 0.66 μM. iZMYND8-34 inhibits the binding of H3K4me1–H3K14ac peptide to the ZMYND8 protein. iZMYND8-34 inhibits ZMYND8’s histone recognition. iZMYND8-34 blocks neuroendocrine prostate cancer development .
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- HY-100014
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Histone Demethylase
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Cancer
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KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B) .
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- HY-P2255
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Histone Demethylase
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Others
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H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci .
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- HY-100764
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YUKA1
1 Publications Verification
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Histone Demethylase
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Cancer
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YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers .
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- HY-138691A
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JADA82 trihydrochloride; PCK82 trihydrochloride
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Histone Demethylase
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Cancer
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JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma .
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- HY-149091
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Histone Demethylase
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Cancer
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KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs .
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- HY-158432
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Histone Demethylase
PROTACs
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Cancer
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GT-653 is a PROTAC degrader for lysine-specific demethylase 5B (KDM5B). GT-653 degrades 68.35% KDM5B at 10 μM in a ubiquitin proteasome-dependent manner, upregulates H3K4me3 levels, and activates the type-I interferon signaling pathway in prostate cancer cells 22RV1. (Pink: KDM5B ligand (HY-158433); Black: Linker (HY-W004896); Blue: E3 ligase ligand (HY-103596))
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- HY-N0857
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GLUT
HDAC
Virus Protease
PI3K
AMPK
Akt
Histone Demethylase
MDM-2/p53
IFNAR
Reactive Oxygen Species (ROS)
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Infection
Metabolic Disease
Inflammation/Immunology
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Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a KD of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescence and virus infection .
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- HY-15313C
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Histone Demethylase
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Metabolic Disease
Cancer
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CBB1007 trihydrochloride is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 trihydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 trihydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 trihydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .
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- HY-128912
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Histone Demethylase
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Cancer
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Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity .
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- HY-125837A
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Epigenetic Reader Domain
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Cancer
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MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells .
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- HY-138691
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JADA82; PCK82
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Histone Demethylase
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Cancer
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JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma .
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- HY-P2257
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Histone Demethylase
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Others
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H3K4(Me3) (1-20) is a histone peptide. Trimethylation of histone H3 on lysine 4 (H3K4 me3) is found in active euchromatin but not in silent heterochromatin .
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- HY-150619
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Histone Demethylase
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Cancer
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KDM4-IN-4 (compound 47) is a potent histone lysine demethylase 4 (KDM4) inhibitor with a modest affinity binding to ~80 μM for KDM4A-Tudor domain. KDM4-IN-4 can inhibit H3K4Me3 binding to the Tudor domain in cells with an EC50 value of 105 μM. KDM4-IN-4 can be used for researching anticancer .
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- HY-15313B
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Histone Demethylase
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Metabolic Disease
Cancer
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CBB1007 hydrochloride is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 hydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 hydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 hydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .
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- HY-15313
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Histone Demethylase
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Metabolic Disease
Cancer
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CBB1007 is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .
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- HY-138691B
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JADA82 dihydrochloride; PCK82 dihydrochloride
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Histone Demethylase
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Cancer
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JQKD82 (JADA82) dihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 dihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma .
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- HY-179229
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PROTACs
Histone Demethylase
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Cancer
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LSD1-IN-47 is a highly efficient PROTAC degrader targeting LSD1 (IC50 = 43 nM). LSD1-IN-47 does not alter LSD1 protein levels and does not increase the histone marker H3K4me2. LSD1-IN-47 can be used for the study of colon carcinoma .
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- HY-176283
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Microtubule/Tubulin
Histone Demethylase
Apoptosis
Wee1
Bcl-2 Family
Caspase
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Cancer
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Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells .
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- HY-149213
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J54; J3-54
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Histone Demethylase
TLK
Apoptosis
PD-1/PD-L1
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Cancer
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LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC50 of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer .
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- HY-125837
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Epigenetic Reader Domain
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Cancer
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MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells .
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- HY-179339
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Histone Demethylase
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Cancer
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LSD1-IN-46 is a potent and orally active Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.082 μM. LSD1-IN-46 interrupts the β-catenin-mediated transcriptional program, thereby suppressing the stemness of gastric cancer cells. LSD1-IN-46 exhibits strong anti-tumor activity. LSD1-IN-46 can be used for the research of gastric cancer .
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- HY-173590
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Histone Demethylase
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Cancer
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AW4 is a LSD1 inhibitor. AW4 inhibits LSD1 ΔTTAS activity in H3K4me2 demethylation assays. AW4 can be used for research of drug resistance .
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- HY-168086
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PD-1/PD-L1
Histone Demethylase
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Infection
Inflammation/Immunology
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LSD1-IN-35 (Compound Z-1) is a selective LSD1 Inhibitor (IC50: 108 nM). LSD1-IN-35 inhibits the demethylation on H3K4me1/2. LSD1-IN-35 is an immunomodulator. LSD1-IN-35 promotes response of gastric cancer cells to T-cell killing effect by decreasing PD-L1 expression and further attenuates the PD-1/PD-L1 interaction .
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- HY-P10819
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Histone Demethylase
Apoptosis
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Cancer
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S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
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- HY-168968S
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EGFR
Histone Demethylase
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Cancer
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ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
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- HY-181781
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Histone Demethylase
CD44
Apoptosis
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Cancer
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LSD1-IN-48 is a tranylcypromine-pyrimidine derivative and selective LSD1 inhibitor with a human IC50 of 7.87 nM. LSD1-IN-48 increases H3K4me1/2 histone methylation levels. LSD1-IN-48 induces apoptosis, upregulates CD86, downregulates SOX2 and CD44, inhibits proliferation in cancer cells. LSD1-IN-48 can be used for the research of acute myeloid leukemia .
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- HY-183603
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DNA/RNA Synthesis
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Cancer
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FRC-222 is a CHD1 tandem chromodomain inhibitor with a Kd of 0.15 μM and an IC50 of 0.18 μM. FRC-222 binds to the H3K4me3 binding site of CHD1 tandem chromodomain via aromatic cage interactions and extended ligand contacts. FRC-222 can be used for the research of prostate cancer[1].
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- HY-148829
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WDR5
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Cancer
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MS40 is a WDR5 PROTAC degrader (Kd = 125 nM). MS40 promotes the ubiquitination and degradation of WDR5. MS40-induced WDR5 degradation leads to the dissociation of the MLL/KMT2A complex from chromatin, resulting in decreased H3K4me2 levels. MS40 can be used in the study of primary leukemia .
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- HY-121511
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Epigenetic Reader Domain
Wnt
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Cancer
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EML631 is a SPIN1 inhibitor with a Kd of 3-7 μM. EML631 interacts with the second Tudor domain of SPIN1 and blocks its ability to read the H3K4me3 histone mark. EML631 inhibits the coactivator activity of SPIN1 in the Wnt signaling pathway and reduces the activity of Wnt response reporter genes. EML631 can be used in cancer-related research .
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- HY-183602
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DNA/RNA Synthesis
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Cancer
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FRC-303 is a CHD1 inhibitor with a Kd of 0.14 μM and an IC50 of 0.18 μM. FRC-303 binds to the H3K4me3 binding site of CHD1 tandem chromodomain, forms aromatic cage interactions and extended ligand contacts, acts as a methyl-lysine mimic, and occupies natural peptide ligand-binding regions. FRC-303 can be used for the research of prostate cancer .
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- HY-100421R
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Histone Demethylase
Reference Standards
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Cancer
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CPI-455 (Standard) is the analytical standard of CPI-455 (HY-100421). This product is intended for research and analytical applications. CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
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- HY-100764R
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Histone Demethylase
Reference Standards
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Cancer
|
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YUKA1 (Standard) is the analytical standard of YUKA1 (HY-100764). This product is intended for research and analytical applications. YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers .
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- HY-183105
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Histone Demethylase
Apoptosis
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Cancer
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DC551040 is an orally active and selective lysine demethylase 1 (LSD1) inhibitor with a human IC50 of 2.14 nM. DC551040 binds to LSD1 via π-π stacking with Trp552, polar interactions with Phe538, and covalent adduct formation with FAD, and disrupts the LSD1-GFI1B-CoREST complex. DC551040 induces H3K4me2 accumulation, apoptosis, and cell differentiation, activates STAT5, NF-κB, AKT, and IL6-STAT3 pathways, and upregulates IL6 expression. DC551040 can be used for the research of acute myeloid leukemia .
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- HY-100014R
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Histone Demethylase
Reference Standards
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Cancer
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KDM5A-IN-1 (Standard) is the analytical standard of KDM5A-IN-1 (HY-100014). This product is intended for research and analytical applications. KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B) .
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| Cat. No. |
상품명 |
Target |
Research Area |
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- HY-P2255
-
|
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Histone Demethylase
|
Others
|
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H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci .
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- HY-P2256
-
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Peptides
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Others
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H3K4(Me2) (1-20) is a histone peptide. H3K4me2 regulates the recovery of protein biosynthesis and homeostasis following DNA damage .
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- HY-P2257
-
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Histone Demethylase
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Others
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H3K4(Me3) (1-20) is a histone peptide. Trimethylation of histone H3 on lysine 4 (H3K4 me3) is found in active euchromatin but not in silent heterochromatin .
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- HY-P10819
-
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Histone Demethylase
Apoptosis
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Cancer
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S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
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| Cat. No. |
상품명 |
Category |
Target |
Chemical Structure |
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- HY-N0857
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Structural Classification
Acanthaceae
Simsia foetida (Cav.) S.F.Blake
Terpenoids
Diterpenoids
Plants
Source Classification
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GLUT
HDAC
Virus Protease
PI3K
AMPK
Akt
Histone Demethylase
MDM-2/p53
IFNAR
Reactive Oxygen Species (ROS)
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Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a KD of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescence and virus infection .
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- HY-128912
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Alkaloids
Animals
Source Classification
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Histone Demethylase
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Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity .
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| Cat. No. |
상품명 |
Chemical Structure |
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- HY-168968S
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ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity .
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