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Chromatin/Epigenetic

DNA Methyltransferase

(40)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(77)

Histone Acetyltransferase

(48)

Histone Demethylase

(93)

Histone Methyltransferase

Methionine Adenosyltransferase (MAT)

Histone 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).

Filter HomeSignaling PathwaysChromatin/EpigeneticHistone Demethylase

KDM4-IN-4

T603542230475-63-3In house

KDM4-IN-4 (compound 47) is a potent inhibitor of histone lysine demethylase 4 (KDM4), with a binding constant of approximately 80 μM for the KDM4A-Tudor domain. It inhibits H3K4Me3 binding to the Tudor domain in cellular contexts with an EC50 value of 105 μM, holding potential for anticancer research applications [1].

278 €

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Zavondemstat

T701211851412-93-5In house

Zavondemstat (QC8222 free base) is a histone lysine demethylase 4 (KDM4) inhibitor with anticancer and antitumor activity for the study of triple-negative and breast cancers.

144 €

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T-448

T130571597426-53-3In house

T-448 is a specific, orally active, and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) with an IC50 of 22 nM.

432 €

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Eicosapentaenoic Acid

T536810417-94-4

Eicosapentaenoic Acid (EPA) is a ω-3 fatty acid abundantly available in marine organisms.

64 €

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GSK-J4 Hydrochloride

T43831797983-09-5

GSK-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.

32 €

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GSK467

T54841628332-52-4

GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).

59 €

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Bomedemstat ditosylate

T700081990504-72-7In house

Bomedemstat 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.

111 €

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AS8351

T4100796-42-9

AS8351 (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.

40 €

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GSK-J4

T31001373423-53-0In house

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3 me2 demethylases JMJD3 KDM6B and UTX KDM6A (IC50=8.6 6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

48 €

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JIB-04

T1868199596-05-9

JIB-04 (NSC 693627) is a pan-selective Jumonji histone demethylase inhibitor.

28 €

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Pulrodemstat benzenesulfonate

T118822097523-60-7

Pulrodemstat benzenesulfonate (CC-90011 benzenesulfonate) is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity.

52 €

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CPI-455

T35521628208-23-0

CPI-455 is a specific KDM5 inhibitor.

35 €

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KDM2A/7A-IN-1

T117482169272-46-0In house

KDM2A 7A-IN-1 is a cell-permeable and selective inhibitor of histone lysine demethylase KDM2A 7A, with potential antitumor activity for studying duodenal adenomas and ossifying fibromucoid tumors.

258 €

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GSK-LSD1 dihydrochloride

T23152102933-95-7

GSK-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).

32 €

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3-pyridine toxoflavin

T6773832502-20-8

3-pyridine toxoflavin is a potent KDM4C inhibitor, IC50=19nM.

185 €

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TAK-418

T392521818252-53-7In house

TAK-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.

133 €

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OG-L002

T60731357302-64-7

OG-L002 is an effective and selective LSD1 inhibitor (IC50: 20 nM), showing 69- and 36-fold selectivity over MAO-A and MAO-B, respectively.

33 €

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ORY1001

T69221431326-61-2

ORY1001 (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.

51 €

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Corin

T108641808113-09-8In house

Corin is an irreversible inhibitor of HDAC1(IC50 = 147 nM) and LSD1(Ki = 110 nM).

170 €

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KDM1A-IN-29

T888341423715-30-3

KDM1A-IN-29 is a histone demethylase inhibitor.

185 €

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LSD1-IN-20

T631401239589-91-3In house

Lsd1-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.

377 €

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KDM2B-IN-2

T393891965248-01-4

KDM2B-IN-2 is a potent histone demethylase (kdm2b) inhibitor.

57 €

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Ryuvidine

T23284265312-55-8

Ryuvidine is a dual inhibitor of KDM5A and SETD8, an inducer of the DNA damage response with potential anticancer activity, inhibition of H4K20 methylation, and inhibition of CDK4, and can be used to study breast cancer and erythroplasia.

57 €

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IOX1

T65455852-78-8

IOX1 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.

36 €

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Pulrodemstat

T392581821307-10-1In house

Pulrodemstat (CC-90011) is an orally active, selective, and highly efficient lysine-specific demethylase-1 (LSD1) inhibitor with anticancer activity. It inhibits HNSCC cell proliferation and migration by triggering apoptosis and inhibiting head and neck squamous cell carcinoma growth.

278 €

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KDM5-C70

T156481596348-32-1

KDM5-C70 is an ethyl ester derivative of KDM5-C49 and functions as an effective, cell-permeable, pan-KDM5 histone demethylase inhibitor. It exhibits an antiproliferative effect in myeloma cells and induces a genome-wide elevation of H3K4me3 levels.

35 €

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GSK-LSD1

T822541431368-48-7

GSK-LSD1 is a selective LSD1 inhibitor with potential anticancer activity that attenuates the expression of CTGF CCN2, MMP13, LOXL4, and waveform proteins in cancer cells.GSK-LSD1 regulates the cell cycle, induces apoptosis, and can be used to study breast cancer.

28 €

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NCGC00244536

TQ00502003260-55-5

NCGC00244536 (KDM4B Inhibitor B3) is a potent KDM4B inhibitor (IC50: 10 nM).

92 €

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Seclidemstat

T45271423715-37-0

Seclidemstat (SP-2577) is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.

38 €

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KDM5-IN-1

T156491628210-26-3

KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.

55 €

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Tranylcypromine (2-PCPA) hydrochloride

T10251986-47-6

Tranylcypromine (2-PCPA) hydrochloride (SKF-385 HCl), a Monoamine Oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression.

37 €

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Tranylcypromine hemisulfate

T794213492-01-8

Tranylcypromine hemisulfate (Tranylcypromine Sulfate) is an inhibitor of monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1) with a rapid onset of activity.

45 €

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SD49-7

T6778154009-54-0

SD49-7 is an inhibitor of histone lysine demethylase 4 (KDM4) with an IC50 of 0.19 µM.

52 €

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PBIT

T164352514-30-9

PBIT inhibits JARID1B histone demethylase (IC50 of about 3 μM). PBIT also inhibits JARID1A and JARID1C (IC50s of 6 μM and 4.9 μM, respectively). PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes .

32 €

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PFI-90

T924353995-62-3

PFI-90, a selective histone demethylase (KDM3B) inhibitor, targets PAX3-FOXO1 action and demonstrates potential antitumor activity. It induces apoptosis and myogenic differentiation, leading to increased cell death.

32 €

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DDP-38003 dihydrochloride

T10983L1831167-98-6In house

DDP-38003 dihydrochloride is an orally available histone lysine-specific demethylase 1A (KDM1A LSD1) inhibitor (IC50: 84 nM).

69 €

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GSK-J1

T68471373422-53-7

GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases.

38 €

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L-2-Hydroxyglutaric acid disodium

T1374863512-50-5

L-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).

42 €

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KDM4C-IN-1

T6065452348-60-4

KDM4C-IN-1 is a selective and potent KDM4C inhibitor (IC50: 8 nM) with potential anticancer activity.KDM4C-IN-1 inhibits the growth of HepG2 and A549 cells, and can be used for the study of leukaemia.

94 €

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FY-21

T77583 In house

FY-21 is a selective LSD1 inhibitor (IC50= 340 nM) that inhibits proliferation and colony formation of leukemia cells, decreases mRNA levels of the transcription factors HOXA9 and MEIS1, and can be used in the study of leukemia.

185 €

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5-Hydroxy-7-acetoxy-8-methoxyflavone

TN312095480-80-1

5-Hydroxy-7-acetoxy-8-methoxyflavone is a flavonoid compound that inhibits lipid peroxidation and may exhibit anti-influenza virus activity.

235 €

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GSK2879552 2HCl (1401966-69-5(free base))

T4418

GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

51 €

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KDM5A-IN-1

T156501905481-36-8

KDM5A-IN-1 is an orally available, potent and selective inhibitor of the pan-histidine lysine demethylase 5 KDM5, inhibiting KDM5A, KDM5B, and KDM5C with IC50 values of 45 nM, 56 nM, and 55 nM, respectively.KDM5A-IN-1 inhibits PC9 H3K4Me3, and may be useful in cancer research.

141 €

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Daminozide

T37191596-84-5

Daminozide (Succinic Acid) is a plant growth regulator, selectively inhibits the KDM2 7 JmjC subfamily.

39 €

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LSD1-IN-27

T776352904571-94-2

LSD1-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.

150 €

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ML324

T65931222800-79-4

ML324(IC50=920 nM) is a specific inhibitor of jumonji histone demethylase (JMJD2).

44 €

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RN-1 dihydrochloride

T216521781835-13-9

RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM).

39 €

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HDAC3-IN-T247

T241311451042-18-4

HDAC3-IN-T247 (HDAC3 inhibitor T247) is a selective and potent histone deacetylase 3 (HDAC3) inhibitor with anticancer and antiviral activities.HDAC3-IN-T247 induces NF-κB acetylation in human colon cancer HCT116 cells in a dose-dependent manner.HDAC3-IN-T247 inhibits cancer cell proliferation. HDAC3-IN-T247 inhibits cancer cell proliferation.

79 €

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