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Chromatin/Epigenetic

DNA Methyltransferase

(45)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(82)

Histone Acetyltransferase

(51)

Histone Demethylase

(96)

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].

$293

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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.

$152

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Eicosapentaenoic Acid

T536810417-94-4

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

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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.

$455

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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.

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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.

$117

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GSK467

T54841628332-52-4

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

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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.

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CPI-455

T35521628208-23-0

CPI-455 is a specific KDM5 inhibitor.

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JIB-04

T1868199596-05-9

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

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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.

$272

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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.

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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.

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Corin

T108641808113-09-8In house

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

$179

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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.

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3-pyridine toxoflavin

T6773832502-20-8

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

$195

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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).

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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.

$140

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YUKA1

T17278708991-09-7

YUKA1, a cell-permeable KDM5A inhibitor (IC50=2.66 μM) with a weak effect on KDM5C (IC50=7.12 μM) and no effect on other KDM isoforms, was able to increase the level of H3K4me3 in human cells and inhibit the proliferation of cancer cells, and also prevented the emergence of drug-resistant cells.

$370

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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.

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KDM1A-IN-29

T888341423715-30-3

KDM1A-IN-29 is a histone demethylase inhibitor.

$195

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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.

$397

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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.

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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.

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