Histone Demethylase

Histone Demethylase Related Products (133):

By Effects:	Inhibitors (104) Activators (4) Degraders (5) Controls (2)

Cat. No.	Product Name	Effect	Purity

HY-B0568

Deferiprone	Inhibitor	99.98%
Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study.

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-138794

XL177A	Inhibitor	99.60%
XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections.

HY-B1018A

Phenelzine sulfate	Inhibitor	99.96%
Phenelzine sulfate, an antidepressant agent, is an irreversible and orally active monoamine oxidase (MAO-A and MAO-B) inhibitor. Phenelzine sulfate inhibits GABA transaminase and primary amine oxidase (PrAO), and sequester reactive aldehydes. Phenelzine sulfate also inhibits LSD1 (Ki: 5.6 μM) and suppresses oxidative stress and lipogenesis. Phenelzine sulfate elevates neurotransmitters (serotonin, norepinephrine, dopamine). Phenelzine sulfate is studied in neurological, metabolic and cancer diseases for depression and anxiety disorders, stroke, spinal cord injury, traumatic brain injury, multiple sclerosis, Parkinson’s disease, Alzheimer’s disease, inflammatory pain, obesity and prostate cancer.

HY-139782

SKLB325	Inhibitor	99.21%
SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (K_D) value of 0.755 μM, and the IC₅₀ value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) .

HY-178825A

LD-110 triTFA	Degrader	99.56%
LD-110 triTFA is a highly efficient and effective LSD1 PROTAC degrader (DC₅₀ = 0.44 μM). LD-110 triTFA promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 triTFA inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 triTFA can be used for the study of esophagus squamous cancer.

HY-178825B

LD-110 trihydrochloride	Degrader
LD-110 trihydrochloride is a highly efficient and effective LSD1 PROTAC degrader (DC₅₀ = 0.44 μM). LD-110 trihydrochloride promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 trihydrochloride inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 trihydrochloride can be used for the study of esophagus squamous cancer.

HY-179610

YU185530	Inhibitor
YU185530 is a JARID1 histone demethylase inhibitor.

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.

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-162275

JMJD1C-IN-1	Inhibitor	99.96%
JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC₅₀ = 0.59 μM, K_d = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC₅₀ = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells.

HY-B0546

Procaine		99.79%
Procaine is a DNA-demethylating agent. Procaine acts through multiple targets and has a slow onset and a short duration of action.

HY-12315

N-Oxalylglycine	Inhibitor	99.18%
N-Oxalylglycine (N-Oxaloglycine) is a Jumonji C-domain-containing histone lysine demethylase inhibitor. N-Oxalylglycine inhibits JMJD2A, JMJD2C and JMJD2D. N-Oxalylglycine also inhibits HIF prolylhydroxylase domain-1 (PHD-1) and PHD-2, with an IC₅₀ of 2.1 μM and 5.6 μM, respectively.

HY-112623

Vafidemstat	Inhibitor	98.03%
Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.

HY-129079

TFMB-(R)-2-HG	Inhibitor	98.26%
TFMB-(R)-2-HG is a cell membrane-permeable (R)-2-HG and acute myeloid leukemia (AML) oncogenic factor. TFMB-(R)-2-HG competitively inhibits α-ketoglutarate-dependent dioxygenases such as KDM2B and FTO. TFMB-(R)-2-HG impairs cell differentiation in response to Estrogen withdrawal. TFMB-(R)-2-HG is used in acute myeloid leukemia and glioma research.

HY-Q36392

JNJ-9350	Inhibitor	99.21%
JNJ-9350, a chemical probe, is an inhibitor of spermine oxidase (SMOX) with an IC₅₀ value of 0.01 μM. JNJ-9350 also inhibits polyamine oxidase (PAO) with an IC₅₀ value of 0.79 μM. JNJ-9350 can be used for the research of cancer.

HY-15221

Methylstat	Inhibitor	99.85%
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis.

HY-W017132

2,4-PDCA	Inhibitor	99.82%
2,4-PDCA (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-PDCA is a target chemical in the field of bio-based plastics.

HY-139434

JMJD6-IN-1	Inhibitor	99.51%
JMJD6-IN-1 is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM. JMJD6-IN-1 inhibits MCF-7 and HCC4006 cell proliferation with IC₅₀ values of 19.2 μM and 25.2 μM. JMJD6-IN-1 inhibits JMJD6 demethylase activity. JMJD6-IN-1 can be used for the research of lung adenocarcinoma, prostate cancer, breast cancer, pancreatic cancer, colon cancer, oral squamous cell carcinoma, and glioblastoma.

HY-110130

RN-1 dihydrochloride	Inhibitor	99.21%
RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC₅₀ of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC₅₀ values of 0.51 μM and 2.785 μM respectively.

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