Histone-Demethylase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html Histone HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html DemethylaseThere are two classes of enzymes involved in histone methylation: methyltransferases and de

2、methylases. While methyltransferasesare responsible for establishing methylation patterns, demethylases are capable of removing methyl groups not only from histonesbut other proteins as well. Histone demethylases not only target methylated sites on histone tails but also interact with methylatedsite

3、s on non-histone proteins, such as p53.Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and theirtight associations with diseases including cancer and mental disorders.JMJD1A (also named KDM3A) is a demethylasethat removes met

4、hyl from histone lysine H3K9. It plays important roles in variouscellular processes, including spermatogenesis, energy metabolism, regulation of stem cell and gender display.Jumonji domain-containing 3 (Jmjd3) has been identified as a histone demethylase, which specifically catalyzes the removal ofm

5、ethylation from H3K27me3.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html Histone HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html Demethylase HYPERLINK https:/www.MedChemE/Targets/Histone Demet

6、hylase.html HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html Antagonists HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html HYPERLINK ht

7、tps:/www.MedChemE/Targets/Histone Demethylase.html & HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html HYPERLINK https:/www.MedChemE/Targets/Histone Demethylase.html Activators HYPERLINK https:/www.MedChemE/rel-tranylcypromine-d5-hydrochloride.html (rel)-Tranylcypromine HYPERLINK https:

8、/www.MedChemE/rel-tranylcypromine-d5-hydrochloride.html HYPERLINK https:/www.MedChemE/rel-tranylcypromine-d5-hydrochloride.html D5 HYPERLINK https:/www.MedChemE/rel-tranylcypromine-d5-hydrochloride.html HYPERLINK https:/www.MedChemE/rel-tranylcypromine-d5-hydrochloride.html hydrochloride(2-Phenylcyc

9、lopropylamine D5 hydrochloride) Cat. No.: HY-17447SA HYPERLINK https:/www.MedChemE/2-4-pdca.html 2,4-PDCACat. No.: HY-W017132(rel)-Tranylcypromine D5 hydrochloride(2-Phenylcyclopropylamine D5 hydrochloride) is adeuterium labeled (rel)-Tranylcyprominehydrochloride.2,4-PDCA (2,4 pyridine dicarboxylic

10、acid) is abroad-spectrum inhibitor of 2OG oxygenase,including JmjC domain-containing family ofhistone demethylases (JHDMs). 2,4-PDCA is atarget chemical in the field of bio-basedplastics.Purity: 98%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize:

11、 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AS8351.html AS8351(NSC51355) Cat. No.: HY-100744 HYPERLINK https:/www.MedChemE/bizine.html BizineCat. No.: HY-121095AS8351 (NSC51355) is a KDM5B inhibitor, whichcan induce and sustain active chromatin marks tofacilitate the induction of cardiomyocyte-likecel

12、ls.Bizine, a Phenelzine analogue, is a potent andselective LSD1 inhibitor, with a bK of 59 nM.iBizine can modulate bulk histone methylation incancer cells. Bizine shows neuroprotectiveeffects.Purity: 99.89%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%C

13、linical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bomedemstat.html Bomedemstat(IMG-7289) Cat. No.: HY-109169 HYPERLINK https:/www.MedChemE/bomedemstat-ditosylate.html Bomedemstat HYPERLINK https:/www.MedChemE/bomedemstat-ditosylate.html HYPERLINK https:/www.MedChemE

14、/bomedemstat-ditosylate.html ditosylate(IMG-7289 ditosylate) Cat. No.: HY-109169ABomedemstat (IMG-7289) is an orally active andirreversible inhibitor of the epigeneticallyactive lysine-specific demethylase 1 (LSD1) inmouse models of myeloproliferative neoplasms(MPNs).Bomedemstat (IMG-7289) ditosylat

15、e is an oral andirreversible inhibitor of the epigeneticallyactive lysine-specific demethylase 1 (LSD1) inmouse models of myeloproliferative neoplasms(MPNs).Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize:

16、1 mg, 5 mg HYPERLINK https:/www.MedChemE/cbb1003.html CBB1003 HYPERLINK https:/www.MedChemE/cbb1003.html HYPERLINK https:/www.MedChemE/CBB1003-hydrochloride.html CBB1003 HYPERLINK https:/www.MedChemE/CBB1003-hydrochloride.html HYPERLINK https:/www.MedChemE/CBB1003-hydrochloride.html hydrochlorideCat

17、. No.: HY-15774 Cat. No.: HY-15774ACBB1003 is a novel histone demethylase LSD1inhibitor with IC50 of 10.54 uM. IC50 value: 10.54uM Target: LSD1 inhibitor in vitro: Treatment ofF9 cells with CBB1003 led to the activation ofCHRM4 and SCN3A expression.CBB1003 Hcl is a novel histone demethylase LSD1inhi

18、bitor with IC50 of 10.54 uM. IC50 value: 10.54uM Target: LSD1 inhibitor in vitro: Treatment ofF9 cells with CBB1003 led to the activation ofCHRM4 and SCN3A expression.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HY

19、PERLINK https:/www.MedChemE/cbb1007.html CBB1007 HYPERLINK https:/www.MedChemE/cbb1007.html HYPERLINK https:/www.MedChemE/CBB1007-hydrochloride.html CBB1007 HYPERLINK https:/www.MedChemE/CBB1007-hydrochloride.html HYPERLINK https:/www.MedChemE/CBB1007-hydrochloride.html hydrochlorideCat. No.: HY-153

20、13 Cat. No.: HY-15313BCBB1007 is a cell-permeable amidino-guanidiniumcompound that acts as a potent, reversible andsubstrate competitive LSD1 selective inhibitor(IC50 = 5.27 M for hLSD1).CBB1007 Hcl is a cell-permeableamidino-guanidinium compound that acts as apotent, reversible and substrate compet

21、itive LSD1selective inhibitor (IC50 = 5.27 M for hLSD1).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/CBB1007

22、-trihydrochloride.html CBB1007 HYPERLINK https:/www.MedChemE/CBB1007-trihydrochloride.html HYPERLINK https:/www.MedChemE/CBB1007-trihydrochloride.html trihydrochloride HYPERLINK https:/www.MedChemE/CBB1007-trihydrochloride.html HYPERLINK https:/www.MedChemE/Corin.html CorinCat. No.: HY-15313C Cat. N

23、o.: HY-111048CBB1007 trihydrochloride is a cell-permeableamidino-guanidinium compound that acts as apotent, reversible and substrate competitive LSD1selective inhibitor (IC50 = 5.27 M for hLSD1).Corin is a dual inhibitor of histone lysinespecific demethylase (LSD1) and histonedeacetylase (HDAC), wit

24、h a K(inact) of 110 nMifor LSD1 and an IC of 147 nM for HDAC1.50Purity: 96.58%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.75%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/CPI-455.html

25、CPI-455 HYPERLINK https:/www.MedChemE/CPI-455.html HYPERLINK https:/www.MedChemE/daminozide.html DaminozideCat. No.: HY-100421 Cat. No.: HY-13643CPI-455 is a specific, pan-KDM5 inhibitor withan IC of 10 nM for KDM5A.50Daminozide, a plant growth regulator, is aselective inhibitor of the human KDM2/7

26、histonedemethylases, with IC s of 0.55, 1.5 and 2.150M for PHF8, KDM2A, and KIAA1718, respectively.Purity: 98.95%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 500 mg, 1 g, 5 g HYPERLINK ht

27、tps:/www.MedChemE/DDP-38003-dihydrochloride.html DDP-38003 HYPERLINK https:/www.MedChemE/DDP-38003-dihydrochloride.html HYPERLINK https:/www.MedChemE/DDP-38003-dihydrochloride.html dihydrochloride HYPERLINK https:/www.MedChemE/DDP-38003-dihydrochloride.html HYPERLINK https:/www.MedChemE/DDP-38003_tr

28、ihydrochloride.html DDP-38003 HYPERLINK https:/www.MedChemE/DDP-38003_trihydrochloride.html HYPERLINK https:/www.MedChemE/DDP-38003_trihydrochloride.html trihydrochlorideCat. No.: HY-19612A Cat. No.: HY-19612BDDP-38003 dihydrochloride is an novel, orallyavailable inhibitor of histone lysine-specific

29、demethylase 1A (KDM1A/LSD1) with an IC of 8450nM.DDP-38003 trihydrochloride is an novel, orallyavailable inhibitor of histone lysine-specificdemethylase 1A (KDM1A/LSD1) with an IC of 8450nM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 96.77%Clinical Data: No Development R

30、eportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Eicosapentaenoic-Acid.html Eicosapentaenoic HYPERLINK https:/www.MedChemE/Eicosapentaenoic-Acid.html HYPERLINK https:/www.MedChemE/Eicosapentaenoic-Acid.html Acid HYPERLINK https:/www.MedChemE/Eicosapentaenoic-Ac

31、id.html HYPERLINK https:/www.MedChemE/eicosapentaenoic-acid-sodium.html Eicosapentaenoic HYPERLINK https:/www.MedChemE/eicosapentaenoic-acid-sodium.html HYPERLINK https:/www.MedChemE/eicosapentaenoic-acid-sodium.html Acid HYPERLINK https:/www.MedChemE/eicosapentaenoic-acid-sodium.html HYPERLINK http

32、s:/www.MedChemE/eicosapentaenoic-acid-sodium.html sodium(EPA; Timnodonic acid) Cat. No.: HY-B0660 (EPA sodium; Timnodonic acid sodium) Cat. No.: HY-W011269Eicosapentaenoic Acid (EPA) is an orally activeOmega-3 long-chain polyunsaturated fatty acid (-3LC-PUFA).Eicosapentaenoic Acid (EPA)sodium is an

33、orallyactive Omega-3 long-chain polyunsaturated fattyacid (-3 LC-PUFA).Purity: 95.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mg, 500 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/eicosapentaenoic-acid-d5.html Eicosapentaenoic HYPERLINK https:/www.MedCh

34、emE/eicosapentaenoic-acid-d5.html HYPERLINK https:/www.MedChemE/eicosapentaenoic-acid-d5.html Acid-d5 HYPERLINK https:/www.MedChemE/eicosapentaenoic-acid-d5.html HYPERLINK https:/www.MedChemE/GSK_690_Hydrochloride.html GSK HYPERLINK https:/www.MedChemE/GSK_690_Hydrochloride.html HYPERLINK https:/www

35、.MedChemE/GSK_690_Hydrochloride.html 690 HYPERLINK https:/www.MedChemE/GSK_690_Hydrochloride.html HYPERLINK https:/www.MedChemE/GSK_690_Hydrochloride.html Hydrochloride(EPA-d5; Timnodonic acid-d5) Cat. No.: HY-B0660SCat. No.: HY-117226AEicosapentaenoic Acid-d5 (EPA-d5) is the deuteriumlabeled Eicosa

36、pentaenoic Acid. EicosapentaenoicAcid (EPA; Timnodonic acid) is an omega-3 fattyacid.GSK 690 (Hydrochloride) is a reversible inhibitorof lysine specific demethylase 1 (LSD1), with aKd IC50value of 9 nM and a biochemical of 37nM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity:

37、 99.16%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/GSK-J1.html GSK-J1 HYPERLINK https:/www.MedChemE/GSK-J1.html HYPERLINK https:/www.MedChemE/GSK-J1-lithium-salt.html GSK-J1 HYPERLINK https:/www.MedChemE/GSK-J1

38、-lithium-salt.html HYPERLINK https:/www.MedChemE/GSK-J1-lithium-salt.html lithium HYPERLINK https:/www.MedChemE/GSK-J1-lithium-salt.html HYPERLINK https:/www.MedChemE/GSK-J1-lithium-salt.html saltCat. No.: HY-15648 Cat. No.: HY-15648DGSK-J1 is a potent inhibitor ofH3K27me3/me2-demethylases JMJD3/KDM

39、6BUTX/KDM6A, with IC of 60 nM towards50KDM6B. .andGSK-J1 lithium salt is a potent inhibitor ofH3K27me3/me2-demethylases JMJD3/KDM6B andUTX/KDM6A, with IC of 60 nM towards KDM6B.50Purity: 99.76%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data

40、: No Development ReportedSize: 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/GSK-J4.html GSK-J4 HYPERLINK https:/www.MedChemE/GSK-J4.html HYPERLINK https:/www.MedChemE/gsk-j4-hydrochloride.html GSK-J4 HYPERLINK https:/www.MedChemE/gsk-j4-hydrochloride.html HYPERLINK https:/www.MedChemE/g

41、sk-j4-hydrochloride.html hydrochlorideCat. No.: HY-15648B Cat. No.: HY-15648FGSK-J4 is a potent dual inhibitor ofH3K27me3/me2-demethylases JMJD3/KDM6B andUTX/KDM6A with IC s of 8.6 and 6.6 M,50respectively. GSK-J4 inhibits LPS-induced TNF-production in human primary macrophages with anIC of 9 M.50Pu

42、rity: 99.64%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgGSK-J4 hydrochloride is a potent dual inhibitor ofH3K27me3/me2-demethylases JMJD3/KDM6B andUTX/KDM6A with IC s of 8.6 and 6.6 M,50respectively. GSK-J4 hydrochloride inhibitsLPS-induced TNF- production in human primarymac

43、rophages with an IC of 9 M.50Purity: 98.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/GSK-LSD1_Dihydrochloride.html GSK-LSD1 HYPERLINK https:/www.MedChemE/GSK-LSD1_Dihydrochloride.html HYPERLINK https:/www.MedChemE/GSK-LSD1_Dihydrochloride.html

44、 dihydrochloride HYPERLINK https:/www.MedChemE/GSK-LSD1_Dihydrochloride.html HYPERLINK https:/www.MedChemE/gsk-lsd1-d4-dihydrochloride.html GSK-LSD1-d4 HYPERLINK https:/www.MedChemE/gsk-lsd1-d4-dihydrochloride.html HYPERLINK https:/www.MedChemE/gsk-lsd1-d4-dihydrochloride.html dihydrochlorideCat. No

45、.: HY-100546A Cat. No.: HY-100546ASGSK-LSD1 dihydrochloride is a potent, selectiveand irreversible lysine specific demethylase 1(LSD1) inhibitor with an IC of 16 nM.50GSK-LSD1-d4 dihydrochloride is the deuteriumlabeled GSK-LSD1 dihydrochloride. GSK-LSD1dihydrochloride is a potent, selective andirrev

46、ersible lysine specific demethylase 1 (LSD1)inhibitor with an IC of 16 nM.50Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/GSK2879552.html GSK2879552 HYPERLI

47、NK https:/www.MedChemE/GSK2879552.html HYPERLINK https:/www.MedChemE/gsk2879552-dihydrochloride.html GSK2879552 HYPERLINK https:/www.MedChemE/gsk2879552-dihydrochloride.html HYPERLINK https:/www.MedChemE/gsk2879552-dihydrochloride.html dihydrochlorideCat. No.: HY-18632 Cat. No.: HY-18632AGSK2879552

48、an orally active, selective andirreversible inhibitor of lysine specificdemethylase 1 (LSD1/ KDM1A), with potentialantineoplastic activity.GSK2879552 dihydrochloride an orally active,selective and irreversible inhibitor of lysinespecific demethylase 1 (LSD1/KDM1A), withpotential antineoplastic activ

49、ity.Purity: 98%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.52%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/gsk467.html GSK467 HYPERLINK https:/www.MedChemE/gsk467.html HYPERLINK https:/www.MedChemE/hdac6-in-3.html H

50、DAC6-IN-3Cat. No.: HY-116761 Cat. No.: HY-145259GSK467 is a cell penetrant and selective KDM5B(JARID1B or PLU1) inhibitor with a K of 10 nM,ishows 180-fold selectivity for KDM4C and nomeasurable inhibitory effects toward KDM6 or otherJumonji family members.HDAC6-IN-3 (Compound 14), an antiprostate c

51、anceragent, is a potent, orally active HDAC6 inhibitorwith IC s ranging from 0.02-1.54 M for50HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effectiveMAO-A (IC50=0.79 M) and LSD1 inhibitor.Purity: 98.14%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Da

52、ta: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/ORY-1001_trans_.html Iadademstat HYPERLINK https:/www.MedChemE/ORY-1001_trans_.html HYPERLINK https:/www.MedChemE/ORY-1001_trans_.html dihydrochloride HYPERLINK https:/

53、www.MedChemE/ORY-1001_trans_.html (ORY-1001 dihydrochloride; RG6016dihydrochloride; RO 7051790 dihydrochloride) Cat. No.: HY-12782T HYPERLINK https:/www.MedChemE/incb059872.html INCB059872Cat. No.: HY-141677Iadademstat (ORY-1001) dihydrochloride is aselective irreversible lysine (K)-specificdemethyl

54、ase 1A (KDM1A/LSD1) inhibitor.INCB059872 is a potent, orally active, selectiveand irreversible Lysine-Specific Demethylase 1(LSD1) inhibitor. INCB059872 can be used for theresearch of myeloid leukemia.Purity: 98.30%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical

55、 Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/IOX1.html IOX1 HYPERLINK https:/www.MedChemE/IOX1.html HYPERLINK https:/www.MedChemE/JIB-04.html JIB-04Cat. No.: HY-12304 Cat. No.: HY-13953IOX1, 5-Carboxy-8-hydroxyquinoline, is a potentbroadspectrum inhibitor of 2OG oxyge

56、nases,including the JmjC demethylases. IOX1 inhibitsKDM4C, KDM4E, KDM2A, KDM3A and KDM6B with ICvalues of 0.6 M, 2.3 M, 1.8 M, 0.1 M and 1.4M, respectively. IOX1 also inhibits ALKBH5.50JIB-04 is a pan-selective Jumonji histonedemethylase inihibitor with IC s of 230, 340,50855, 445, 435, 1100, and 29

57、0 nM for JARID1A,JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D,respectively.Purity: 99.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98.12%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChe

58、mE/jmjd7-in-1.html JMJD7-IN-1Cat. No.: HY-132198 HYPERLINK https:/www.MedChemE/jada82.html JQKD82(JADA82; PCK82) Cat. No.: HY-138691JMJD7-IN-1 is a potent JMJD7 inhibitor, with anIC of 6.62 M. JMJD7-IN-1 shows good inhibitory50activity against cells expressing a high level ofJMJD7.JQKD82 (JADA82) is

59、 a cell-permeable and selectiveKDM5 inhibitor. JQKD82 increases H3K4me3 andcan be used for the research of multiple myeloma.Purity: 98.07%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLI

60、NK https:/www.MedChemE/kdm2-7-in-1.html KDM2/7-IN-1 HYPERLINK https:/www.MedChemE/kdm2-7-in-1.html HYPERLINK https:/www.MedChemE/kdm2a-7a-in-1.html KDM2A/7A-IN-1Cat. No.: HY-107573 Cat. No.: HY-108706KDM2/7-IN-1 (TC-E 5002) is a selective histonedemethylase KDM2/7 subfamily inhibitor (IC50values are