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Histone Demethylase

Histone Demethylase

Cat. No. Product Name CAS No. Information
CSN26665 T-448 free base 1597426-52-2 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].
CSN20393 T-3775440 hydrochloride 1422535-52-1 T-3775440 is an LSD1 inhibitor which inhibits SCLC cell proliferation by disrupting LDS1 interactions with SNAG domain proteins INSM1 and GFI1B.
CSN15764 SP2509 1423715-09-6 SP-2509 is a histone demethylase LSD1 KDM1A antagonist with IC50 of 13 nM
CSN21313 Seclidemstat 1423715-37-0 Seclidemstat is an LSD1 inhibitor with mean IC50 value of 127nM.
CSN26667 S2157 2262488-39-9 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].
CSN26666 S2116 2262489-89-2 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].
CSN23851 QC6352 1851373-36-8 QC-6352 is a selective inhibitor of KDM4 family with IC50s of 104 nM, 56 nM, 35 nM, and 104 nM for KDM4A, KDM4B, KDM4C and KDM4D respectively.
CSN51373 PFI-90 53995-62-3 PFI-90 is a selective inhibitor of histone demethylase (KDM3B).
CSN26407 PBIT 2514-30-9 PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM. PBIT also inhibits JARID1A and JARID1C with IC50 values of 6 and 4.9 μM, respectively[1].
CSN21131 Iadademstat dihydrochloride 1431303-72-8 ORY-1001 trans is a selective irreversible lysine K-specific demethylase 1A KDM1ALSD1 inhibitor
CSN16347 Iadademstat (ORY-1001) 2HCl 1431326-61-2 ORY-1001 is a selective inhibitor of lysine-specific demethylase LSD1KDM1A with IC50 of 20 nM
CSN17182 OG-L002 1357302-64-7 OG-L002 is a selective inhibitor of LSD1 with IC50 of 20 nM
CSN19732 NCL-1 2199214-20-3 NCL-1 is a KDM1A-specific inhibitor to promote differentiation and apoptosis of glioma stem cells GSCs KDM1A inhibitor modulates several pathways related to stemness differentiation and apoptosis it can induce activation of the unfolded protein response UPR pathway
CSN21362 NCGC00247743 1435192-04-3 NCGC00247743 is a histone lysine demethylase KDM4 inhibitor
CSN21075 NCGC00244536 2003260-55-5 NCGC00244536 is a selective inhibitor of KDM4A with IC50 of 10 nM
CSN19733 NCD-38 1456907-39-3 NCD-38 is a KDM1A-specific inhibitor to promote differentiation and apoptosis of glioma stem cells GSCs KDM1A inhibitor modulates several pathways related to stemness differentiation and apoptosis it can induce activation of the unfolded protein response UPR pathway
CSN13837 ML324 1222800-79-4 ML324 is an inhibitor of JMJD2 demethylase with IC50 of 920 nM with antiviral activity
CSN20246 LPE-1 1637373-70-6 LPE-1 is a histone lysine specific demethylase 1 LSD1 IC5003360003M inhibitor selectively suppressed the viability of esophageal cancer cell line EC-109 bearing overexpressed LSD1 It can significantly suppressed proliferation induced apoptosis arrested cell cycle of EC109 cells at G2M phase and caused changes of the associated protein markers correspondingly
CSN27531 L-2-Hydroxyglutaric acid disodium 63512-50-5 L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
CSN18063 KDM5A-IN-1 1905481-36-8 KDM5A-IN-1 is an inhibitor of histone demethylases.
CSN26160 KDM5-IN-1 1628210-26-3 KDM5-IN-48 is a potent, selective and orally bioavailable KDM5 inhibitor with IC50 value of 15.1nM. It improved H3K4Me3 level with EC50 value of 0.34μM in PC9 cells.
CSN29559 JMJD7-IN-1 311316-96-8 JMJD7-IN-1 is a potent JMJD7 inhibitor with IC50 value of 6.62μM.
CSN13708 JIB-04   199596-05-9 JIB-04 is a selective inhibitor of jumonji histone demethylase with IC50s of 2303408554454351100 and 290 nM for JARID1AJMJD2EJMJD3JMJD2AJMJD2BJMJD2C and JMJD2D respectively
CSN12941 IOX1   5852-78-8 IOX1 is the broad-spectrum inhibitor of 2OG oxygenases and its IC50 for KDM4AKDM3A and KDM4CKDM6BKDM2AKDM4E are 0601 M and 06 M16 M18 M23 M
CSN23888 GSK467 1628332-52-4 GSK467 is a selective KDM5 inhibitor with Ki of 10 nM. It has no measurable inhibitory effects toward other JmJ family members.
CSN13902 GSK2879552 1401966-69-5 GSK2879552 is an irreversible inhibitor of lysine specific demethylase 1 LSD1 with Ki of 17 M with antineoplastic activity
CSN19211 GSK2879552 dihydrochloride 1902123-72-1 GSK2879552 2HCl is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
CSN19181 GSK-J4 hydrochloride   1797983-09-5 GSK-J4 HCl is selective inhibitor of jumonji H3K27 demethylase. It can attenuate lipopolysaccharide (LPS)-induced proinflammatory cytokine production.
CSN17785 GSK-J2 1394854-52-4 GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 IC50 100 M making it an appropriate negative control for in vitro studies involving GSK-J1 and is a selective inhibitor for human H3K27me3 demethylases
CSN18962 GSK-J1 lithium salt 1373422-39-9 GSK-J1 lithium is a potent and selective inhibitor of the H3K27 histone demethylases JMJD3 and UTX IC50 60 nM for human JMJD3 in vitro
CSN13832 GSK-J1 1373422-53-7 GSK-J1 is a H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM for JMJD3 KDM6B and UTX KDM6A respectively
CSN16348 GSK-J4 1373423-53-0 GSK J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor and attenuates lipopolysaccharide (LPS)-induced proinflammatory cytokine production in primary human macrophages (IC50 9 M for the inhibition of TNF release).
CSN18965 DDP-38003 dihydrochloride 1831167-98-6 DDP-38003 2HCl is an orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
CSN16898 CPI-455   1628208-23-0 CPI-455 is a selective inhibitor of KDM5 demethylases and can reduce survival of drug-tolerant cancer cells
CSN19243 CPI-455 HCl   2095432-28-1 CPI-455 HCl is an inhibitor of KDM5 It can elevate global levels of H3K4 trimethylation H3K4me3 and decrease the number of DTPs in multiple cancer cell line models
CSN23733 Corin 1808113-09-8 Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
CSN25222 Pulrodemstat benzenesulfonate 2097523-60-7 CC-90011 is a potent and orally active LSD1 inhibitor. It is in phase I clinical study of CC-90011 in patients (pts) with advanced unresectable solid tumors and R/R NHL.
CSN17765 CBB1007 1379573-92-8 CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent reversible and substrate competitive LSD1 selective inhibitor IC50 527 M for hLSD1
CSN18959 CBB1007 HCl 2070014-96-7 CBB1007 HCl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
CSN18960 CBB1007 trihydrochloride 2070015-03-9 CBB1007 3HCl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
CSN17764 CBB1003 1379573-88-2 CBB1003 is a histone demethylase LSD1 inhibitor with IC50 of 1054 M
CSN18963 CBB1003 HCl 2070015-02-8 CBB1003 HCl is a histone demethylase LSD1 inhibitor with IC50 of 10.54 μM.
CSN21279 AS8351   796-42-9 AS8351 is a selective inhibitor of histone demethylase KDM5B JARID1B via competing for the chelated iron KDM5B needs and it can act as an iron chelator
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