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].
α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
QC6352 is a potent KDM4C inhibitor with an IC50 of 35 nM.
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][2].
SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with IC50 of 13 nM.
GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
α-Hydroxyglutaric acid-13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[1].
Fenoldopam (SKF 82526) hydrochloride is a D1 receptor agonist and a novel lysine-specific demethylase 1 (LSD1) inhibitor (IC50=0.8974 μM). Fenoldopam hydrochloride shows anti-hypertensive effects, anti-cancer cell proliferation activity and can induce cells apoptosis[1][2][3].
KDM5-C49 is a potent, selective KDM5 inhibitor with IC50 of 25, 30 and 59 nM for KDM5A, B and C, respectively; displays 25-100-fold selectivity over KDM6B, 2-30-fold selectivity over KDM4 family, but with less cell-permeablity.
KDM5B-IN-3 (Compound 5) is a histone lysine specific demethylase 5B (KDM5B/JARID1B) inhibitor with an IC50 of 9.32 μM. KDM5B-IN-3 can be used for the research of gastric cancer[1].
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity[1].
Bomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity[1].
LSD1-IN-13 (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 induces differentiation of AML (acute myeloid leukemia) cell lines[1].
JMJD6-IN-1 (Compound 1-3) is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM. JMJD6-IN-1 inhibits MCF-7 and HCC4006 cell proliferation with IC50s of 19.2 μM and 25.2 μM. JMJD6-IN-1 can be used for research of cancers[1].
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].
HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity[1].
CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.IC50 value: 10.54 uM [1]Target: LSD1 inhibitorin vitro: Treatment of F9 cells with CBB1003 led to the activation of CHRM4 and SCN3A expression. Treatment of CBB1003 led to significant growth inhibition of mouse embryonic teratocarcinoma F9 cells. Treatment of mouse ES cells with CBB1003 and 1007 also led to substantial inhibition of the spherical growth of ES cells [1]. CBB1003 inhibited CRC cell proliferation and colony formation. In cultured CRC cells, inhibiting LSD1 activity by CBB1003 caused a decrease in LGR5 levels while overexpression of LGR5 reduced CBB1003-induced cell death [2].
CPI-455 is a specific KDM5 inhibitor.
Vafidemstat is a dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.
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].
GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
LSD1-IN-24(compound 3S) is a selective LSD1 inhibitor with IC50 = 0.247 μM. LSD1-IN-24 can mediate the expression of PD-L1, enhance T cell killing response, and can be used in cancer research[1].
T-448 is a specific and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons[1].
KDM4-IN-4 (compound 47) is a potent histone lysine demethylase 4 (KDM4) inhibitor with a modest affinity binding to ~80 μM for KDM4A-Tudor domain. KDM4-IN-4 can inhibit H3K4Me3 binding to the Tudor domain in cells with an EC50 value of 105 μM. KDM4-IN-4 can be used for researching anticancer[1].
CPI-4203 is a potent KDM5A inhibitor with an IC50 of 250 nM. CPI-4203 is competitive with 2-oxoglutarate (2-OG). CPI-4203 is structurally related to CPI-455 (HY-100421) but is less potent[1].
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][2].
T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons[1].
NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.
GSK467 is a selective KDM5 (JARID1) inhibitor with a Ki of 10 nM for KDM5B, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members[1].