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Chromatin/Epigenetic
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Chromatin/EpigeneticHistone Demethylase
Histone demethylase proteins have a variety of domains that serve different functions. These functions include binding to the histone (or sometimes the DNA on the nucleosome), recognizing the correct methylated amino acid substrate and catalyzing the reaction, and binding cofactors. Cofactors include: alpha-keto glutarate (JmjC-domain containing demethylases), CoREST (LSD), FAD, Fe (II) or NOG (N-oxalylglycine).
- 3-pyridine toxoflavinT6773832502-20-83-pyridine toxoflavin is a potent KDM4C inhibitor, IC50=19nM.
- $195
SizeQTY
- 5-Hydroxy-7-acetoxy-8-methoxyflavoneTN312095480-80-15-Hydroxy-7-acetoxy-8-methoxyflavone is a flavonoid compound that inhibits lipid peroxidation and may have anti-influenza virus activity.
- $248
SizeQTY - LSD1-IN-20T631401239589-91-3In houseLsd1-in-20 is a potent dual inhibitor of LSD1/G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.
- $397
SizeQTY - Acetyl Pentapeptide-1 acetateT38318LAcetyl Pentapeptide-1 acetate is an histone deacetylase inhibitor.
- $148
SizeQTY - LSD1-IN-27T776352904571-94-2LSD1-IN-27 is a potent LSD1 inhibitor with an IC50 value of 13 nM.LSD1-IN-27 inhibited the stemness and migration of gastric cancer cells.LSD1-IN-27 inhibited the expression of PD-L1 in BGC-823 and MFC cells.LSD1-IN-27 potentiated the T-cell immune response against gastric cancer.
- $195
SizeQTY - KDM5-C49 HClT27723LKDM5-C49 HCl (KDOAM-20 hydrochloride) is a potent and selective inhibitor of KDM5 demethylase. KDM5-C49 HCL(1596348-16-1 Free base) is a candidate compound for the treatment of cancer.
- $195
SizeQTY - GSK2879552 2HCl (1401966-69-5(free base))T4418GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
- $54
SizeQTY
Cited - DDP-38003 dihydrochlorideT10983L1831167-98-6In houseDDP-38003 dihydrochloride is an orally available histone lysine-specific demethylase 1A (KDM1A/LSD1) inhibitor (IC50: 84 nM).
- $73
SizeQTY - CorinT108641808113-09-8In houseCorin is an irreversible inhibitor of HDAC1(IC50 = 147 nM) and LSD1(Ki = 110 nM).
- $179
SizeQTY - GSK-J4T31001373423-53-0In houseGSK-J4 (GSK J4 HCl) is a potent H3K27me3 demethylase inhibitor, with IC50s of 8.6 μM and 6.6 μM towards KDM6B and KDM6A respectively. It is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.
- $51
SizeQTY Cited - QC6352T167001851373-36-8In houseQC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).
- $1,520
SizeQTY - KDM2A/7A-IN-1T117482169272-46-0In houseKDM2A/7A-IN-1 is a cell-permeable and selective inhibitor of the histone lysine demethylase KDM2A/7A with potential antitumor activity for the study of duodenal adenomas and ossifying fibromucoid tumors.
- $272
SizeQTY - $272
- T-448T130571597426-53-3In houseT-448 is a specific, orally active and irreversible lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) inhibitor(IC50 of 22 nM).
- $1,970
SizeQTY - TAK-418T392521818252-53-7In houseTAK-418 is a selective and orally active inhibitor of LSD1/KDM1A enzyme with an IC50 of 2.9 nM. TAK-418 unlocks abnormal epigenetic mechanisms and improves autism symptoms in models of neurodevelopmental disorders.
- $233
SizeQTY - Bomedemstat ditosylateT700081990504-72-7In houseBomedemstat ditosylate (IMG-7289 ditosylate) is an orally active lysine-specific demethylase 1 (LSD1) inhibitor with antitumor activity that potentiates the response to PD-1 inhibition in a homozygous model of SCLC, inhibits cancer cell proliferation, and induces apoptosis. Bomedemstat ditosylate can be used to study myeloproliferative neoplasms and myelofibrosis.
- $117
SizeQTY - ORY1001T69221431326-61-2ORY1001 (ORY 1001) is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor, with high selectivity against related FAD dependent aminoxidases with IC50 of <20 nM.
- $54
SizeQTY Cited - AS8351T4100796-42-9AS8351 (NSC51355) is a histone demethylase inhibitor. It has been used in combination with CHIR99021, A 83-01, BIX01294, SC-1, Y-27632, OAC2, SU 16f, and JNJ-10198409 to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.
- $43
SizeQTY Cited - GSK-LSD1T822541431368-48-7GSK-LSD1, an LSD1 inhibitor, decreases food consumption and body weight while enhancing insulin sensitivity and glycemic regulation in murine obesity models. Additionally, it mitigates non-alcoholic fatty liver disease (NAFLD) and suppresses cytokine release induced by SARS-CoV-2 in COVID-19 peripheral blood mononuclear cells (PBMCs). Furthermore, GSK-LSD1 inhibits the proliferation and spread of cancer [1] [2] [3].
- Inquiry Price
SizeQTY - T-3775440 hydrochlorideT130551422535-52-1T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).
- $97
SizeQTY - LSD1-IN-30T839661289575-45-6LSD1-IN-30 is a lysine-specific demethylase 1 (LSD1) inhibitor with anticancer activity for the study of small cell lung cancer and acute myeloid leukemia.
- $118
SizeQTY - GSK J5T228211394854-51-3GSK J5 is an inhibitor of schistosomes and helminths and is often used as a trematode insecticide.GSK J5 promotes schistosome mortality in a dose- and time-dependent manner.GSK J5 increases the mortality rate of schistosomes and decreases the viability of adult worms.GSK J5 is an inhibitor of schistosomes and helminths and is often used as a trematode insecticide.
- $39
SizeQTY - JQKD82T399892410512-38-6JQKD82 is a selective inhibitor of KDM5 and increases H3K4me3. JQKD82 can be used in studies about the treatment of multiple myeloma.
- $137
SizeQTY - LSD1-IN-24T678714734-59-2LSD1-IN-24 is a selective and potent LSD1 inhibitor with an IC50 value of 0.247 μM.LSD1-IN-24 induces PD-L1 expression and enhances the T cell killing response, and can be used in cancer-related diseases.
- $73
SizeQTY - KDM2B-IN-2T393891965248-01-4KDM2B-IN-2 is a potent histone demethylase (kdm2b) inhibitor.
- $60
SizeQTY - SD49-7T6778154009-54-0SD49-7 is an inhibitor of histone lysine demethylase 4 (KDM4) with an IC50 of 0.19 µM.
- $55
SizeQTY - KDM4D-IN-1T42142098902-68-0KDM4D-IN-1 is a KDM4D inhibitor (IC50: 0.41±0.03 μM).
- $101
SizeQTY - LSD1-IN-25T748552911585-60-7LSD1-IN-25 (Compound 9j) is a potent, selective, and orally active inhibitor of LSD1, exhibiting an IC50 of 46 nM (Ki = 30.3 nM) and capable of inducing apoptosis in cancer cells [1].
- Inquiry Price
SizeQTY - Tranylcypromine hemisulfateT794213492-01-8Tranylcypromine hemisulfate (Tranylcypromine Sulfate) is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1) with a rapid onset of activity.
- $48
SizeQTY - KDM5-IN-1T156491628210-26-3KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.
- $58
SizeQTY - GSK-J4 HydrochlorideT43831797983-09-5GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.
- $34
SizeQTY - L-2-Hydroxyglutaric acid disodiumT1374863512-50-5L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium) is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity(Km and Ki of 2.52 mM and 11.13 mM, respectively).
- $45
SizeQTY - RN-1 dihydrochlorideT216521781835-13-9RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM).
- $48
SizeQTY - SeclidemstatT45271423715-37-0Seclidemstat (SP-2577) is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.
- $41
SizeQTY - IOX1T65455852-78-8IOX1 is the most effective broad-spectrum 2OG oxygenases(including the JmjC demethylases) inhibitor. The IC50 of IOX1 for KDM4A, KDM3A, is 0.6 and 0.1 uM, respectively.
- $38
SizeQTY Cited - DaminozideT37191596-84-5Daminozide (Succinic Acid) is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
- $42
SizeQTY - KDM5-C70T156481596348-32-1KDM5-C70 is an ethyl ester derivative of KDM5-C49. KDM5-C70 is an effective, cell-permeable, and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, inducing a genome-wide elevation of H3K4me3 levels.
- $37
SizeQTY Cited - GSK-LSD1 dihydrochlorideT23152102933-95-7GSK-LSD1 dihydrochloride (GSK-LSD1 2HCl) is a specificity irreversible LSD1 inhibitor (IC50: 16 nM). The selectivity of GSK-LSD1 for LSD1 is >1000 fold over other closely related FAD utilizing enzymes (i.e. MAO-A, LSD2, MAO-B).
- $34
SizeQTY - P3FI-63T84287931596-95-1P3FI-63 is a selective KDM3B inhibitor (IC50: 7 μM) with antitumor activity for the study of fusion-positive rhabdomyosarcoma and other transcriptionally addictive cancers.
- $195
SizeQTY - CPI-455 HClT222992095432-28-1CPI-455 is a specific KDM5 inhibitor with IC50 value of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with target
- $1,520
SizeQTY - GSK-J1 lithium saltT114752309668-29-7GSK-J1 lithium salt is an effective inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with an IC 50 of 60 nM for KDM6B.
- Inquiry Price
SizeQTY - KF 13218T11755127654-03-9KF 13218 is a selective, potent and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.
- $1,520
SizeQTY - T-448 free baseT130561597426-52-2T-448 free base is a specific, orally active and irreversible lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) inhibitor(IC50 of 22 nM).
- $1,820
SizeQTY - ProcaineT002959-46-1Procaine (Vitamin H3) is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.
- $46
SizeQTY - Pulrodemstat benzenesulfonateT118822097523-60-7Pulrodemstat benzenesulfonate (CC-90011 benzenesulfonate) is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity.
- $55
SizeQTY - Iadademstat dihydrochlorideT58251431303-72-8Iadademstat dihydrochloride (ORY-1001(trans)) , a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.
- $38
SizeQTY - GSK467T54841628332-52-4GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
- $74
SizeQTY - ML324T65931222800-79-4ML324(IC50=920 nM) is a specific inhibitor of jumonji histone demethylase (JMJD2).
- $47
SizeQTY - GSK 690 HydrochlorideT115032436760-79-9GSK 690 (Hydrochloride) is a reversible lysine specific demethylase 1 (LSD1) inhibitor with a Kd value of 9 nM and IC 50 of 37 nM.
- $1,450
SizeQTY
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