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LSD1+inhibitor

" in MedChemExpress (MCE) Product Catalog:

90

Inhibitors & Agonists

1

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5

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B1496
    Tranylcypromine hemisulfate
    5+ Cited Publications

    SKF 385 hemisulfate

    		 Monoamine Oxidase Histone Demethylase Neurological Disease Cancer
    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 [1] .
    Tranylcypromine hemisulfate
  • HY-N2037
    Higenamine
    5+ Cited Publications

    Norcoclaurine; Demethyl-Coclaurine

    		 MAP3K MDM-2/p53 Adrenergic Receptor ROS Kinase Apoptosis Cardiovascular Disease Endocrinology
    Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases [1] .
    Higenamine
  • HY-12782T
    Iadademstat dihydrochloride
    5+ Cited Publications

    ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride

    		 Histone Demethylase Cancer
    Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
    Iadademstat dihydrochloride
  • HY-100546A
    GSK-LSD1 dihydrochloride
    Maximum Cited Publications
    13 Publications Verification

    		 Histone Demethylase Monoamine Oxidase Cancer
    GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
    GSK-LSD1 dihydrochloride
  • HY-B0735A
    Fenoldopam mesylate
    4 Publications Verification

    Fenoldopam methanesulfonate; SKF-82526 mesylate

    		 Dopamine Receptor Apoptosis Cardiovascular Disease Cancer
    Fenoldopam mesylate (SKF-82526) is a D1 receptor agonist and a novel lysine-specific demethylase 1 (LSD1) inhibitor (IC50=0.8974 μM). Fenoldopam mesylate shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis [1] .
    Fenoldopam mesylate
  • HY-109169
    Bomedemstat
    3 Publications Verification

    IMG-7289

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [1] .
    Bomedemstat
  • HY-103713
    Seclidemstat
    10+ Cited Publications

    SP-2577

    		 Histone Demethylase Cancer
    Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=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 [1] .
    Seclidemstat
  • HY-N2037A
    Higenamine hydrochloride
    5+ Cited Publications

    Norcoclaurine hydrochloride

    		 MAP3K MDM-2/p53 ROS Kinase Apoptosis Infection Cardiovascular Disease Endocrinology Cancer
    Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases [1] .
    Higenamine hydrochloride
  • HY-19333
    OG-L002
    2 Publications Verification

    		 Histone Demethylase Monoamine Oxidase HSV Infection
    OG-L002 is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 is a potent monoamine oxidases (MAO) inhibitor with IC50s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 potently inhibits the expression of HSV IE genes [1].
    OG-L002
  • HY-110130
    RN-1 dihydrochloride

    		Histone Demethylase Cardiovascular Disease Cancer
    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 [1] .
    RN-1 dihydrochloride
  • HY-109169A
    Bomedemstat ditosylate
    3 Publications Verification

    IMG-7289 ditosylate

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [1] .
    Bomedemstat ditosylate
  • HY-141677
    INCB059872

    		Histone Demethylase Cancer
    INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 can be used for the research of myeloid leukemia [1].
    INCB059872
  • HY-103713A
    Seclidemstat mesylate
    10+ Cited Publications

    SP-2577 mesylate

    		 Histone Demethylase Cancer
    Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate 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 mesylate can be used for the research of Ewing Sarcoma [1] .
    Seclidemstat mesylate
  • HY-103085
    T-3775440 hydrochloride
    3 Publications Verification

    		 Histone Demethylase Cancer
    T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
    T-3775440 hydrochloride
  • HY-110277
    S2101

    		Histone Demethylase Cancer
    S2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s [1].
    S2101
  • HY-109169B
    Bomedemstat hydrochloride
    3 Publications Verification

    IMG-7289 hydrochloride

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [1] .
    Bomedemstat hydrochloride
  • HY-121095
    Bizine

    		Histone Demethylase Neurological Disease Cancer
    Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects [1].
    Bizine
  • HY-141677A
    INCB059872 dihydrochloride

    		Histone Demethylase Cancer
    INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 dihydrochloride can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 dihydrochloride can be used for the research of myeloid leukemia [1].
    INCB059872 dihydrochloride
  • HY-145259
    HDAC6-IN-3

    		HDAC Histone Demethylase Cancer
    HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor [1]. HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HDAC6-IN-3
  • HY-109169C
    Bomedemstat dihydrochloride
    3 Publications Verification

    IMG-7289 dihydrochloride

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [1] .
    Bomedemstat dihydrochloride
  • HY-15313C
    CBB1007 trihydrochloride
    2 Publications Verification

    		 Histone Demethylase Metabolic Disease Cancer
    CBB1007 trihydrochloride is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 trihydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 trihydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 trihydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma [1] .
    CBB1007 trihydrochloride
  • HY-100546
    GSK-LSD1

    		Histone Demethylase Infection Metabolic Disease Cancer
    GSK-LSD1, a chemical probe, is a LSD1 inhibitor. GSK-LSD1 reduces food intake and body weight, and improves insulin sensitivity and glycemic control in mouse models of obesity. GSK-LSD1 also ameliorates NAFLD. GSK-LSD1 inhibits SARS-CoV-2-triggered cytokine release in COVID-19 PBMCs. GSK-LSD1 also inhibits cancer growth and metastasis [1] .
    GSK-LSD1
  • HY-178826
    LSD1-IN-45

    		Ligands for Target Protein for PROTAC Histone Demethylase Inflammation/Immunology Cancer
    LSD1-IN-45 is an LSD1 inhibitor and a ligand for the target protein for PROTAC. LSD1-IN-45 can be used to synthesize PROTAC LD-110 (HY-178825) [1].
    LSD1-IN-45
  • HY-149249
    MY-943

    		Microtubule/Tubulin Apoptosis Histone Demethylase Cancer
    MY-943 is a potent tubulin polymerization and LSD1 inhibitor with anticancer activity. MY-943 induces G2/M phase arrest and apoptosis, and inhibits cell migration. MY-943 can be used for gastric cancer research [1].
    MY-943
  • HY-136522
    S2116

    		Histone Demethylase Apoptosis Cancer
    S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice [1].
    S2116
  • HY-15774
    CBB1003

    		Histone Demethylase Cancer
    CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
    CBB1003
  • HY-77732
    Ticagrelor acetonide

    Isopropylidene ticagrelor

    		 Drug Derivative Cancer
    Ticagrelor acetonide (Isopropylidene ticagrelor) (Compound 7) is a drug intermediate that can be used for the synthesis of lysine-specific demethylase (LSD1) inhibitors [1].
    Ticagrelor acetonide
  • HY-19612
    DDP-38003

    		Histone Demethylase Cancer
    DDP-38003 (Compound 15) is an orally active KDM1A/LSD1 inhibitor with an IC50 value of 84 nM. DDP-38003 exhibits anticancer activity against promyelocytic leukemia [1].
    DDP-38003
  • HY-146380
    S1427

    		Histone Demethylase Cancer
    S1427 is a tranylcypromine-derived LSD1 inhibitor with the IC50 of 390 nM and Ki of 80 nM. S1427 exhibits desirable hERG channel inhibition and microsomal stability profiles. Inhibition of LSD1 partially reduces the proliferation of cancer cells [1].
    S1427
  • HY-149968
    LSD1-IN-25

    		Histone Demethylase Apoptosis Cancer
    LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis [1].
    LSD1-IN-25
  • HY-12645
    NCL1

    		Histone Demethylase Cancer
    NCL1 is a phenylcyclopropylamine (PCPA)-based Lysine-specific demethylase 1 (LSD1) inhibitor. NCL1 selectively inhibits LSD1 in preference to LSD2, with IC50 values of 2.5 and 26 μM for LSD1 and LSD2, respectively [1].
    NCL1
  • HY-149595
    LSD1-UM-109

    		Histone Demethylase Cancer
    LSD1-UM-109 is a ighly potent and reversible LSD1 inhibitor with an IC50 of 3.1 nM. LSD1-UM-109 inhibits cell growth with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line [1].
    LSD1-UM-109
  • HY-155115
    LSD1-IN-27
    1 Publications Verification

    		 Histone Demethylase PD-1/PD-L1 Cancer
    LSD1-IN-27 is an orally active LSD1 inhibitor (IC50: 13 nM). LSD1-IN-27 inhibits the stemness and migration of gastric cancer cells. LSD1-IN-27 also reduces the expression of PD-L1 in BGC-823 and MFC cells. LSD1-IN-27 can enhance T cell immune response in gastric cancer [1].
    LSD1-IN-27
  • HY-149978
    LSD1-IN-26

    		Histone Demethylase Monoamine Oxidase Apoptosis Bcl-2 Family IAP Caspase Cancer
    LSD1-IN-26 (compound 12u) is a potent LSD1 inhibitor, with an IC50 of 25.3 nM. LSD1-IN-26 also inhibits MAO-A (IC50=1234.57 nM) and MAO-B (IC50=3819.27 nM). LSD1-IN-26 significantly induces apoptosis in MGC-803 cells. LSD1-IN-26 can be used for gastric cancer research [1].
    LSD1-IN-26
  • HY-179339
    LSD1-IN-46

    		Histone Demethylase Cancer
    LSD1-IN-46 is a potent and orally active Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.082 μM. LSD1-IN-46 interrupts the β-catenin-mediated transcriptional program, thereby suppressing the stemness of gastric cancer cells. LSD1-IN-46 exhibits strong anti-tumor activity. LSD1-IN-46 can be used for the research of gastric cancer [1].
    LSD1-IN-46
  • HY-175184
    LSD1-IN-44

    		Histone Demethylase Infection
    LSD1-IN-44 (Compound 19) is a LSD1 inhibitor with an IC50 of 0.02  μM for LSD1-CoREST enzymatic complex. LSD1-IN-44 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. LSD1-IN-44 has no significant toxicity to human cells. LSD1-IN-44 can be used for schistosomiasis research [1].
    LSD1-IN-44
  • HY-176254
    LSD1-IN-43

    		Histone Demethylase Amyloid-β Neurological Disease
    LSD1-IN-43 is a highly selective, reversible, orally active and brain-penetrant LSD1 inhibitor with an IC50 value of 0.8 μM. LSD1-IN-43 has low inhibitory activity against MAO-A and MAO-B, two homologs of LSD1. LSD1-IN-43 significantly inhibits Aβ aggregation and enhances Aβ-induced neuronal cell viability. LSD1-IN-43 can be used for the study of Alzheimer’s disease (AD).
    LSD1-IN-43
  • HY-136523
    S2157

    		Histone Demethylase Apoptosis Cancer
    S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells [1].
    S2157
  • HY-N2037R
    Higenamine (Standard)

    Norcoclaurine (Standard); Demethyl-Coclaurine (Standard)

    		 Reference Standards MAP3K MDM-2/p53 Adrenergic Receptor ROS Kinase Apoptosis Cardiovascular Disease Endocrinology
    Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases [1] .
    Higenamine (Standard)
  • HY-15774A
    CBB1003 hydrochloride

    		Histone Demethylase Cancer
    CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
    CBB1003 hydrochloride
  • HY-160183
    LSD1-IN-29

    		Histone Demethylase Cancer
    LSD1-IN-29 (compound 6) is a Lysine specific demethylase 1 (LSD1) inhibitor with the IC50 of 19 nM [1].
    LSD1-IN-29
  • HY-121095A
    Bizine dihydrochloride

    		Histone Demethylase Neurological Disease Cancer
    Bizine dihydrochloride, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine dihydrochloride can modulate bulk histone methylation in cancer cells. Bizine dihydrochloride shows neuroprotective effects [1].
    Bizine dihydrochloride
  • HY-168527
    Acaricide agent 1

    		Histone Demethylase Cancer
    Acaricide agent 1 (Compound 7l) is a potent LSD1 inhibitor. LSD1 exhibits excellent acaricidal activity against egg of T. cinnabarinus with a LC50 of 0.0035 mg/L [1].
    Acaricide agent 1
  • HY-173590
    AW4

    		Histone Demethylase Cancer
    AW4 is a LSD1 inhibitor. AW4 inhibits LSD1 ΔTTAS activity in H3K4me2 demethylation assays. AW4 can be used for research of drug resistance [1].
    AW4
  • HY-151191
    LSD1-IN-22

    		Histone Demethylase Cancer
    LSD1-IN-22 is a potent Lysine-specific demethylase 1 (LSD1) inhibitor with a Ki value of 98 nM. LSD1-IN-22 has anti-proliferative activity against certain cancer cells [1].
    LSD1-IN-22
  • HY-144673
    LSD1-IN-12

    		Histone Demethylase Monoamine Oxidase Cancer
    LSD1-IN-12 (compound 2) is a potent LSD1 inhibitor, with Ki values of 1.1 μM (LSD1), 61 μM (LSD2), 2.3 μM (MAO-A), and 3.5 μM (MAO-B), respectively [1].
    LSD1-IN-12
  • HY-168504
    LSD1-IN-36

    		Histone Demethylase Apoptosis Cancer
    LSD1-IN-36 is a potent LSD1 inhibitor with an IC50 value of 0.8 nM. LSD1-IN-36 induces apoptosis and arrests the cell cycle. LSD1-IN-36 shows antitumor activity [1].
    LSD1-IN-36
  • HY-144755
    MC2652

    		Histone Demethylase Cancer
    MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells [1].
    MC2652
  • HY-163859
    LSD1-IN-33

    		Histone Demethylase Cardiovascular Disease
    LSD1-IN-33 (7d), an orally active LSD1 inhibitor with an IC50 of 4.51 nM, alleviates Ang II-induced NRCFs activation in vitro and reducing pathological myocardial remodeling in TAC-induced cardiac remodeling and heart failure in vivo [1].
    LSD1-IN-33
  • HY-145861
    LSD1-IN-14

    		Histone Demethylase Apoptosis Cancer
    LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells [1].
    LSD1-IN-14

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