HDAC-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/HDAC.html HDACHistone deacetylasesHDAC (Histone deacetylases) are a class of enzymes that remove acetyl groups (O=C-CH3) from an -N-acetyl lysine amino acid onahistone, allowing the histones to wrap the DNA more tightly. This is important because DNA is wrapped

2、 around histones, andDNA expression is regulated by acetylation and de-acetylation. Its action is opposite to that of histone acetyltransferase. HDACproteins are now also called lysine deacetylases (KDAC), to describe their function rather than their target, which also includesnon-histone proteins.

3、Together with the acetylpolyamine amidohydrolases and the acetoin utilization proteins, the histonedeacetylases form an ancient protein superfamily known as the histone deacetylase superfamily.www.MedChemE 12 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Targ

4、ets/HDAC.html HDAC HYPERLINK https:/www.MedChemE/Targets/HDAC.html HYPERLINK https:/www.MedChemE/Targets/HDAC.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/HDAC.html HYPERLINK https:/www.MedChemE/Targets/HDAC.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/HDAC.html HYPERLINK https:

5、/www.MedChemE/Targets/HDAC.html Activators HYPERLINK https:/www.MedChemE/Targets/HDAC.html HYPERLINK https:/www.MedChemE/Targets/HDAC.html & HYPERLINK https:/www.MedChemE/Targets/HDAC.html HYPERLINK https:/www.MedChemE/Targets/HDAC.html Modulators HYPERLINK https:/www.MedChemE/1-alaninechlamydocin.h

6、tml 1-Alaninechlamydocin HYPERLINK https:/www.MedChemE/1-alaninechlamydocin.html HYPERLINK https:/www.MedChemE/1-naphthohydroxamic-acid.html 1-Naphthohydroxamic HYPERLINK https:/www.MedChemE/1-naphthohydroxamic-acid.html HYPERLINK https:/www.MedChemE/1-naphthohydroxamic-acid.html acidCat. No.: HY-P2

7、698 Cat. No.: HY-1305381-Alaninechlamydocin, a cyclic tetrapeptide, is apotent HDAC inhibitor (IC =6.4 nM).501-Alaninechlamydocin induces G2/M cell cyclearrest and apoptosis in MIA PaCa-2 cells.1-Naphthohydroxamic acid (Compound 2) is a potentand selective HDAC8 inhibitor with an IC of 1450M. 1-Naph

8、thohydroxamic acid is more selectivelyfor HDAC8 than class I HDAC1 and class II HDAC6(IC 100 M).50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/2-hexyl-4-p

9、entynoic-acid.html 2-Hexyl-4-pentynoic HYPERLINK https:/www.MedChemE/2-hexyl-4-pentynoic-acid.html HYPERLINK https:/www.MedChemE/2-hexyl-4-pentynoic-acid.html acid()-2-Hexyl-4-pentynoic acid) Cat. No.: HY-118783 HYPERLINK https:/www.MedChemE/Benzenebutyric_acid.html 4-Phenylbutyric HYPERLINK https:/

10、www.MedChemE/Benzenebutyric_acid.html HYPERLINK https:/www.MedChemE/Benzenebutyric_acid.html acid(4-PBA; Benzenebutyric acid) Cat. No.: HY-A02812-Hexyl-4-pentynoic acid ()-2-Hexyl-4-pentynoicacid), valproic acid (VPA) derivative, exhibitspotential roles of HDAC inhibition (IC =13 M)50and HSP70 induc

11、tion. Potent neuroprotectiveeffects.4-Phenylbutyric acid (4-PBA) is an inhibitor ofHDAC and endoplasmic reticulum (ER) stress, usedin cancer and infection research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.98%Clinical Data: LaunchedSize: 500 mg HYPERLINK https:/www.

12、MedChemE/4-phenylbutyric-acid-d11.html 4-Phenylbutyric HYPERLINK https:/www.MedChemE/4-phenylbutyric-acid-d11.html HYPERLINK https:/www.MedChemE/4-phenylbutyric-acid-d11.html acid-d11(4-PBA-d11; Benzenebutyric acid-d11) Cat. No.: HY-A0281S HYPERLINK https:/www.MedChemE/phenylbutyrate.html 5-Phenylpe

13、ntan-2-oneCat. No.: HY-1456134-Phenylbutyric acid-d11 (4-PBA-d11) is thedeuterium labeled 4-Phenylbutyric acid.4-Phenylbutyric acid (4-PBA) is an inhibitor ofHDAC and endoplasmic reticulum (ER) stress, usedin cancer and infection research.5-Phenylpentan-2-one is a potent histonedeacetylases (HDACs)

14、inhibitor.5-Phenylpentan-2-one can be used for urea cycledisorder research.Purity: 98%Clinical Data: No Development ReportedSize: 10 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/PCI-24781.html Abexinostat HYPERLINK h

15、ttps:/www.MedChemE/PCI-24781.html HYPERLINK https:/www.MedChemE/ac-arg-gly-lys-ac-amc.html Ac-Arg-Gly-Lys(Ac)-AMC(CRA 024781; PCI-24781) Cat. No.: HY-10990Cat. No.: HY-P2462Abexinostat (CRA 024781) is a novel pan-HDACinhibitor mostly targeting HDAC1 with K of 7 nM.iAc-Arg-Gly-Lys(Ac)-AMC is a substr

16、ate for HDAC.Purity: 98.61%Clinical Data: Phase 3Size: 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ac-lys-amc.html Ac-Lys-AMC HYPERLINK https:/www.MedChemE/ac-lys-amc.html HYPERLINK https:/www.MedChemE/ACY-1083.html ACY-10

17、83Cat. No.: HY-128919 Cat. No.: HY-111791Ac-Lys-AMC (Hexanamide), also termed MAL, is afluorescent substrate for histone deacetylaseHDACs.ACY-1083 is a selective and brain-penetratingHDAC6 inhibitor with an IC of 3 nM and is50260-fold more selective for HDAC6 than all otherclasses of HDAC isoforms.

18、ACY-1083 effectivelyreverses chemotherapy-induced peripheralneuropathy.Purity: 98.0%Clinical Data:Size: 5 mgPurity: 99.43%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/ACY-738.html ACY-738 HYPERLINK https:/www.MedChemE/

19、ACY-738.html HYPERLINK https:/www.MedChemE/ACY-775.html ACY-775Cat. No.: HY-19327 Cat. No.: HY-19328ACY-738 is a potent, selective andorally-bioavailable HDAC6 inhibitor, with an IC50of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, andHDAC3, with IC s of 94, 128, and 218 nM.50ACY-775 is a potent and s

20、elective inhibitor of theof histone deacetylase 6 (HDAC6) with an IC of507.5nM.Purity: 98.80%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https

21、:/www.MedChemE/ACY-957.html ACY-957 HYPERLINK https:/www.MedChemE/ACY-957.html HYPERLINK https:/www.MedChemE/AES-135.html AES-135Cat. No.: HY-104008 Cat. No.: HY-114483ACY-957 is an orally active and selectiveinhibitor of HDAC1 and HDAC2, with IC s of 750nM, 18 nM, and 1300 nM against HDAC1/2/3,resp

22、ectively, and shows no inhibition onHDAC4/5/6/7/8/9.AES-135, a hydroxamic acid-based pan-HDACinhibitor, prolongs survival in an orthotopicmouse model of pancreatic cancer. AES-135 inhibitsHDAC3, HDAC6, HDAC8, and HDAC11 with IC s ranging50from 190-1100 nM.Purity: 99.87%Clinical Data: No Development

23、ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.31%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/aes-350.html AES-350Cat. No.: HY-138831 HYPERLINK https:/www.MedChemE/alteminostat.html Alteminostat(CKD-581) Cat. No.:

24、 HY-109109AES-350 is a potent and orally active HDAC6inhibitor with an IC50 and a Ki of 0.0244 M and0.035 M, respectively. AES-350 is also againstHDAC3, HDAC8 in an enzymatic activity assay withIC values of 0.187 M and 0.245 M, respectively.50Alteminostat (CKD-581) is a potent HDACinhibitor. Altemin

25、ostat inhibits the class I-IIHDAC family via histone H3 and tubulinacetylation. Alteminostat can be used for lymphomaand multiple myeloma research.Purity: 98.02%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5

26、 mg HYPERLINK https:/www.MedChemE/apicidin.html Apicidin HYPERLINK https:/www.MedChemE/apicidin.html HYPERLINK https:/www.MedChemE/bakkenolide-a.html Bakkenolide HYPERLINK https:/www.MedChemE/bakkenolide-a.html HYPERLINK https:/www.MedChemE/bakkenolide-a.html A(OSI 2040) Cat. No.: HY-N6735Cat. No.:

27、HY-N6017Apicidin (OSI 2040) is a fungal metabolite, actsas a histone deacetylase (HDAC) inhibitor, withantiparasitic activity and a broad spectrumantiproliferative activity.Bakkenolide A is a natural product extracted fromPetasites tricholobus. Bakkenolide A inhibitsleukemia by regulation of HDAC3 a

28、ndPI3K/Akt-related signaling pathways.Purity: 99.87%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/Belinostat.html Belinostat HYPERLINK https:/www.MedChemE/Belinostat.html HYPERLINK https:/www.Me

29、dChemE/BG45.html BG45(PXD101; PX105684) Cat. No.: HY-10225Cat. No.: HY-18712Belinostat (PXD101; PX105684) is a potent HDACinhibitor with an IC of 27 nM in HeLa cell50extracts.BG45 is an HDAC class I inhibitor with selectivityfor HDAC3 (IC50 = 289 nM). It inhibits HDAC1,HDAC2, and HDAC6 with greatly

30、reduced potency(IC50s = 2, 2.2, and 20 M, respectively).Purity: 99.94%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mgPurity: 99.95%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERL

31、INK https:/www.MedChemE/BML-210.html BML-210 HYPERLINK https:/www.MedChemE/BML-210.html HYPERLINK https:/www.MedChemE/BRD_4354.html BRD HYPERLINK https:/www.MedChemE/BRD_4354.html HYPERLINK https:/www.MedChemE/BRD_4354.html 4354Cat. No.: HY-19350 Cat. No.: HY-112719BML-210 is a novel HDAC inhibitor,

32、 and itsmechanism of action has not been characterized.BRD 4354 is a moderately potent inhibitor ofHDAC5 and HDAC9, with IC s of 0.85 and 1.88 M,50respectively.Purity: 96.38%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.29%Clinical Data: No Development

33、ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/brd-4354-ditrifluoroacetate.html BRD HYPERLINK https:/www.MedChemE/brd-4354-ditrifluoroacetate.html HYPERLINK https:/www.MedChemE/brd-4354-ditrifluoroacetate.html 4354 HYPERLINK https:/www.MedChemE/brd-4354-dit

34、rifluoroacetate.html HYPERLINK https:/www.MedChemE/brd-4354-ditrifluoroacetate.html ditrifluoroacetate HYPERLINK https:/www.MedChemE/brd-4354-ditrifluoroacetate.html HYPERLINK https:/www.MedChemE/brd-6929.html BRD-6929Cat. No.: HY-112719B Cat. No.: HY-100719BRD 4354 (ditrifluoroacetate) is a moderat

35、elypotent inhibitor of HDAC5 and HDAC9, with IC s50of 0.85 and 1.88 M, respectively.BRD-6929 is a potent, selectivebrain-penetrant inhibitor of class I histonedeacetylase HDAC1 and HDAC2 inhibitor with ICof 1 nM and 8 nM, respectively.50Purity: 98.06%Clinical Data: No Development ReportedSize: 10 mM

36、 1 mL,Purity: 99.55%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/brd3308.html BRD3308 HYPERLINK https:/www.MedChemE/brd3308.html HYPERLINK https:/www.MedChemE/brd4884.html BRD4884Cat. No.: HY-19618 Cat. No.: HY-102083BRD3308 is a highly selective H

37、DAC3 inhibitorwith an IC of 54 nM. BRD3308 is 23-fold50selectivity for HDAC3 over HDAC1 (IC of 1.2650M) or HDAC2 (IC of 1.34 M).50BRD4884 is a potent HDAC inhibitor with IC50values of 29 nM, 62 nM, and 1.09 M for HDAC1, 2,and 3, respectively.Purity: 98.07%Clinical Data: No Development ReportedSize:

38、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/brd6688.html BRD6688 HYPERLINK https:/www.MedChemE/brd6688.html HYPERLINK https:/www.MedChemE/BRD73954.html BRD73954Cat. No.: HY-117709 Cat. No.: HY-18700BRD6688 is a

39、selective HDAC2 inhibitor. BRD6688increases H4K12 and H3K9 histone acetylation inprimary mouse neuronal cells.BRD73954 ia a potent and selective HDAC inhibitorwith IC50 of 36 nM and 120 nM for HDAC6 and HDAC8,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%

40、Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/bufexamac.html Bufexamac HYPERLINK https:/www.MedChemE/bufexamac.html HYPERLINK https:/www.MedChemE/c-met-hdac-in-2.html c-Met/HDAC-IN-2(Bufexamic acid) Cat. No.: HY-B0494Cat. No.: HY-1434

41、62Bufexamac is a class IIB histone deacetylases(HDAC6 and HDAC10) inhibitor used as ananti-inflammatory agent.c-Met/HDAC-IN-2 is a highly potent c-Met andHDAC dual inhibitor with IC s of 18.49 nM and505.40 nM for HDAC1 and c-Met, respectively.c-Met/HDAC-IN-2 has antiproliferative activitiesagainst c

42、ertain cancer cell lines.Purity: 98.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/CAY10603.html CAY10603(BML-281) Cat. No.: HY-18613 HYPERLINK https:/www.MedChemE/cg347b.html CG34

43、7BCat. No.: HY-135890CAY10603 (BML-281) is a potent and selectiveHDAC6 inhibitor, with an IC of 2 pM; CAY1060350(BML-281) also inhibits HDAC1, HDAC2, HDAC3,HDAC8, HDAC10, with IC s of 271, 252, 0.42, 6851,5090.7 nM.CG347B is a selective HDAC6 inhibitor.Purity: 99.62%Clinical Data: No Development Rep

44、ortedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.84%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 250 mg HYPERLINK https:/www.MedChemE/chdi-390576.html CHDI-390576 HYPERLINK https:/www.MedChemE/chdi-390576.html HYPERLINK https:/www.MedChe

45、mE/chlamydocin.html ChlamydocinCat. No.: HY-119939 Cat. No.: HY-P2228CHDI-390576, a potent, cell permeable and CNSpenetrant class IIa histone deacetylase (HDAC)inhibitor with IC s of 54 nM, 60 nM, 31 nM, 50 nM50for class IIa HDAC4, HDAC5, HDAC7, HDAC9,respectively, shows 500-fold selectivity overcla

46、ss I HDACs (1, 2, 3) and 150-foldChlamydocin, a fungal metabolite, is a highlypotent HDAC inhibitor, with an IC of 1.3 nM.50Chlamydocin exhibits potent antiproliferative andanticancer activities. Chlamydocin inducesapoptosis by activating caspase-3.Purity: 99.42%Clinical Data: No Development Reporte

47、dSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Citarinostat.html Citarinostat(ACY241) Cat. No.: HY-15994 HYPERLINK https:/www.MedChemE/cm-675.html CM-675Cat. No.: HY-114303Citarinostat (ACY241) is a second gener

48、ationpotent, orally active and high-selective HDAC6inhibitor with an IC of 2.6 nM (IC s of 35 nM,50 5045 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3and HDAC8, respectively). Citarinostat hasanticancer effects.CM-675 is a dual phosphodiesterase 5 (PDE5) andclass I histone deacetylases-selective inhi

49、bitor,with IC values of 114 nM and 673 nM for PDE5 and50HDAC1, respectively. CM-675 has potential to treatAlzheimers disease.Purity: 98.57%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.45%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK h

50、ttps:/www.MedChemE/Corin.html Corin HYPERLINK https:/www.MedChemE/Corin.html HYPERLINK https:/www.MedChemE/CRA-026440.html CRA-026440Cat. No.: HY-111048 Cat. No.: HY-19754Corin is a dual inhibitor of histone lysinespecific demethylase (LSD1) and histonedeacetylase (HDAC), with a K(inact) of 110 nMif

51、or LSD1 and an IC of 147 nM for HDAC1.50CRA-026440 is a potent, broad-spectrum HDACinhibitor. The K values against recombinant HDACiisoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8,and HDAC10 are 4, 14, 11, 15, 7, and 20 nMrespectively.Purity: 98.75%Clinical Data: No Development ReportedSize: 10 mM 1 mL

52、, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/crotonoside.html Crotonoside HYPERLINK https:/www.MedChemE/crotonoside.html HYPERLINK https:/www.MedChemE/CUDC-101.html CUDC-101(Isoguanosine) Cat. No.: HY-N0071Cat. No.: HY-10

53、223Crotonoside is isolated from Chinese medicinalherb, Croton. Crotonoside inhibits FLT3 andHDAC3/6, exhibits selective inhibition in acutemyeloid leukemia (AML) cells. Crotonoside could bea promising new lead compound for the treatment ofAML.CUDC-101 is a potent inhibitor of HDAC, EGFR,and HER2 wit

54、h IC s of 4.4, 2.4, and 15.7 nM,50respectively.Purity: 98.18%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 20 mgPurity: 99.19%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg6 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/ww

55、w.MedChemE/HDAC-IN-4.html CXD101 HYPERLINK https:/www.MedChemE/HDAC-IN-4.html HYPERLINK https:/www.MedChemE/cyp51-hdac-in-1.html CYP51/HDAC-IN-1Cat. No.: HY-100748 Cat. No.: HY-144643CXD101 is a potent, selective and orally activeclass I HDAC inhibitor with IC s of 63 nM, 57050nM and 550 nM for HDAC

56、1, HDAC2 and HDAC3,respectively. CXD101 has no activity against HDACclass II. CXD101 has antitumor activity.CYP51/HDAC-IN-1 is a potent, orally activeCYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1inhibits important virulence factors anddown-regulated resistance-associated genes.Purity: 99.71%Clinical Da

57、ta: Phase 2Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Dacinostat.html Dacinostat(NVP-LAQ824; LAQ824) Cat. No.: HY-13606 HYPERLINK https:/www.MedChemE/dihydrochlamydocin.html DihydrochlamydocinCat.

58、No.: HY-115761Dacinostat is a potent HDAC inhibitor, with anIC50 of 32 nM; Dacinostat also inhibits HDAC1with an IC of 9 nM, and used in cancer research.50Dihydrochlamydocin is a histone deacetylases(HDAC) inhibitor. Dihydrochlamydocin shows strongcytostatic activity towards mastocytoma cells.Purity

59、: 98.45%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/4SC-202-free-base.html Domatinostat(4SC-202 free base) Cat. No.: HY-16012A HYPERLINK https:/www.MedChemE/4SC-202.html Domatinost

60、at HYPERLINK https:/www.MedChemE/4SC-202.html HYPERLINK https:/www.MedChemE/4SC-202.html tosylate(4SC-202) Cat. No.: HY-16012Domatinostat (4SC-202 free base) is a selectiveclass I HDAC inhibitor with IC of 1.20 M, 1.1250M, and 0.57 M for HDAC1, HDAC2, and HDAC3,respectively. It also displays inhibit