Histone Demethylase Inhibitor

Histone Demethylase Inhibitors (187):

Cat. No.	Product Name	Effect	Purity

HY-15648B

GSK-J4	Inhibitor	99.64%
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC₅₀s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC₅₀ of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

HY-12304

IOX1	Inhibitor	99.89%
IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC₅₀ values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively. IOX1 also inhibits ALKBH5.

HY-18632

GSK2879552	Inhibitor	99.90%
GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.

HY-100421

CPI-455	Inhibitor	98.95%
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.

HY-168433

LSD1/EGFR-IN-1	Inhibitor
LSD1/EGFR-IN-1 (compound L-1) is a potent inhibitor of LSD1, EGFR^T790M/L858R and EGFR^{L858R/T790M/C797S}, with IC₅₀s of 6.24 and 2.06 and 5.01 μM, respectively. LSD1/EGFR-IN-1 plays an important role in cancer research.

HY-12782T

Iadademstat dihydrochloride	Inhibitor	99.98%
Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.

HY-13953

JIB-04	Inhibitor	98.29%
JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC₅₀s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.

HY-15648

GSK-J1	Inhibitor	99.94%
GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC₅₀ of 60 nM towards KDM6B.

HY-120400

KDM5-C70	Inhibitor
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.

HY-104048

QC6352	Inhibitor	99.13%
QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC₅₀s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC₅₀ of 750 nM (KDM5B).

HY-B1496

Tranylcypromine hemisulfate	Inhibitor	99.94%
Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects.

HY-15648F

GSK-J4 hydrochloride	Inhibitor	99.01%
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC₅₀s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC₅₀ of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1.

HY-100546A

GSK-LSD1 dihydrochloride	Inhibitor	≥98.0%
GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 16 nM.

HY-103713

Seclidemstat	Inhibitor	99.77%
Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (K_i=31 nM, IC₅₀=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma.

HY-116761

GSK467	Inhibitor	99.55%
GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a K_i of 10 nM and an IC₅₀ of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.

HY-100760

Toxoflavin	Inhibitor	99.88%
Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor and antibiotic activity.

HY-111048

Corin	Inhibitor	98.16%
Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a K_i(inact) of 110 nM for LSD1 and an IC₅₀ of 147 nM for HDAC1.

HY-13643

Daminozide	Inhibitor	99.79%
Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC₅₀s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested.

HY-100744

AS8351	Inhibitor	99.88%
AS8351 (NSC51355) is a KDM5B inhibitor, which can induce and sustain active chromatin marks to facilitate the induction of cardiomyocyte-like cells.

HY-18632A

GSK2879552 dihydrochloride	Inhibitor	99.82%
GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.

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