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Histone Demethylase
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| 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 a potent LSD1 inhibitor, with a mean IC50 of 127 nM. |
| 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 (KDM1A/LSD1) inhibitor. |
| CSN16347 | Iadademstat (ORY-1001) 2HCl | 1431326-61-2 | ORY-1001 is a selective inhibitor of lysine-specific demethylase LSD1/KDM1A 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) (IC50=0.336±0.003μM) 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 G2/M 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 230/340/855/445/435/1100, and 290 nM for JARID1A/JMJD2E/JMJD3/JMJD2A/JMJD2B/JMJD2C, and JMJD2D, respectively. |
| CSN12941 | IOX1 | 5852-78-8 | IOX1 is the broad-spectrum inhibitor of 2OG oxygenases and its IC50 for KDM4A/KDM3A and KDM4C/KDM6B/KDM2A/KDM4E are 0.6/0.1 μM and 0.6 μM/1.6 μM/1.8 μM/2.3 μM. |
| 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 1.7 μM 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. |
| CSN19201 | GSK-LSD1 2HCl | 1821798-25-7 | GSK-LSD1 2HCl is a selective LSD1 inhibitor with IC50 of 16 nM. |
| 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 μM), 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 μM for the inhibition of TNFα 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. |
| CSN10740 | Daminozide | 1596-84-5 | Daminozide is a histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.55, 1.5 and 2.1 μM for PHF8, KDM2A and KDM7A respectively). Exhibits ≥ 60-fold selectivity for KDM2/7 demethylases over other histone demethylases and 2-oxoglurate oxygenases (IC50 > 100 μM). |
| 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 = 5.27 μM for hLSD1). |
| CSN18959 | CBB1007 pentahydrochloride | 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 10.54 μM. |
| CSN18963 | CBB1003 HCl | 2070015-02-8 | CBB1003 HCl is a histone demethylase LSD1 inhibitor with IC50 of 10.54 μM. |
| CSN21279 | AS8351 | 329183-01-9 | 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. |
