Aldehyde-Dehydrogenase-ALDH-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html Aldehyde HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html Dehydrogenase HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogen

2、ase (ALDH).html HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html (ALDH)Aldehyde Dehydrogenases (ALDHs) are a superfamily of NADP+-dependent enzymes that metabolize endogenous and exogenousaldehydes to corresponding carboxylic acids. This superfamily of proteins is comprised o

3、f 19 isozymes, with constitutive activity ofat least one isozyme observed in a majority of mammalian tissues. The ALDHs play important roles, among other things, in cellulardetoxification, the protection against ultraviolet radiation-induced damage, and amino acid metabolism.The ALDH1A subfamily pla

4、ys a pivotal role in embryogenesis and development by mediating retinoic acid signaling. ALDH2, as akey enzyme that oxidizes acetaldehyde, is crucial for alcohol metabolism. ALDH1A1 and ALDH3A1 are lens and corneal crystallins,which are essential elements of the cellular defense mechanism against ul

5、traviolet radiation-induced damage in ocular tissues.Many ALDH isozymes are important in oxidizing reactive aldehydes derived from lipid peroxidation and thereby help maintaincellular homeostasis. Increased expression and activity of ALDH isozymes have been reported in various human cancers and area

6、ssociated with cancer relapse. As a direct consequence of their significant physiological and toxicological roles, inhibitors of theALDH enzymes have been developed to treat human diseases.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html Aldehyde HYPERLINK http

7、s:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html Dehydrogenase HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html (ALDH) H

8、YPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).ht

9、ml Agonists HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html & HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH).html HYPERLINK https:/www.MedChemE/Targets/Aldehyde Dehydrogenase (ALDH)

10、.html Antagonists HYPERLINK https:/www.MedChemE/3-hydroxybenzaldehyde.html 3-Hydroxybenzaldehyde HYPERLINK https:/www.MedChemE/3-hydroxybenzaldehyde.html HYPERLINK https:/www.MedChemE/4-diethylaminobenzaldehyde.html 4-DiethylaminobenzaldehydeCat. No.: HY-76006 Cat. No.: HY-W0166453-Hydroxybenzaldehy

11、de is a precursorcompound for phenolic compounds, such asProtocatechualdehyde (HY-N0295).3-Hydroxybenzaldehyde is a substrate of aldehydedehydrogenase (ALDH) in rats and humans (ALDH2).4-Diethylaminobenzaldehyde is a reversible aldehydedehydrogenases (ALDHs) inhibitor, with a K of 4inM for ALDH1. 4-

12、Diethylaminobenzaldehyde displayspotent anti-androgenic effect (IC = 1.71M).50Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mgPurity: 98.82%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/4-hydroxynonenal.html 4-Hydroxynonenal(4

13、-HNE) Cat. No.: HY-113466 HYPERLINK https:/www.MedChemE/4-hydroxynonenal-d3.html 4-Hydroxynonenal-d3(4-HNE-d3) Cat. No.: HY-113466S4-Hydroxynonenal (4-HNE) is an , unsaturatedhydroxyalkenal and an oxidative/nitrosative stressbiomarker. 4-Hydroxynonenal is a substrate and aninhibitor of acetaldehyde

14、dehydrogenase 2 (ALDH2).4-Hydroxynonenal-d3 (4-HNE-d3) is the deuteriumlabeled 4-Hydroxynonenal. 4-Hydroxynonenal (4-HNE)is an , unsaturated hydroxyalkenal and anoxidative/nitrosative stress biomarker.Purity: 99.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clinic

15、al Data:Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Alda-1.html Alda-1 HYPERLINK https:/www.MedChemE/Alda-1.html HYPERLINK https:/www.MedChemE/aldh1a1-in-2.html ALDH1A1-IN-2Cat. No.: HY-18936 Cat. No.: HY-126003Alda-1 is a potent and selective ALDH2 agonist,which activates wild-type ALDH2 and res

16、tores nearwild-type activity to ALDH2*2.ALDH1A1-IN-2 is a potent inhibitor of aldehydedehydrogenase 1a1 (aldh1a1). Aldehydedehydrogenases (ALDH) constitute a family ofenzymes that play a critical role in oxidizingvarious cytotoxic xenogenic and biogenicaldehydes.Purity: 99.99%Clinical Data: No Devel

17、opment ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/aldh1a2-in-1.html ALDH1A2-IN-1 HYPERLINK https:/www.MedChemE/aldh1a2-in-1.html HYPERLINK https:/www.MedChemE/aldh1a3-in-

18、1.html ALDH1A3-IN-1Cat. No.: HY-139031 Cat. No.: HY-144667ALDH1A2-IN-1 is an active site-directed reversibleALDH1A2 inhibitor (IC50=0.91 M; Kd=0.26 M)with several hydrophobic interactions.ALDH1A3-IN-1 (Compound 14) is a potent ALDH1A3inhibitor, with an IC of 0.63 M and a of50 Ki0.46 M. ALDH1A3-IN-1

19、can be studied in prostatecancer.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/aldh1a3-in-3.html ALDH1A3-IN-3 HYPERLINK https:/www.MedChemE/aldh1a3-in-3.html HYPERLINK https:/www.MedChe

20、mE/bodipy-aminoacetaldehyde.html BODIPY HYPERLINK https:/www.MedChemE/bodipy-aminoacetaldehyde.html HYPERLINK https:/www.MedChemE/bodipy-aminoacetaldehyde.html aminoacetaldehydeCat. No.: HY-W017186(BAAA) Cat. No.: HY-136594ALDH1A3-IN-3 (compound 16) is a potent inhibitorof ALDH1A3, with an IC of 0.2

21、6 M. ALDH1A3-IN-350is also a good ALDH3A1 substrate. ALDH1A3-IN-3 canbe used for the research of prostate cancer.BODIPY aminoacetaldehyde (BAAA) is a fluorescentsubstrate for both murine and human aldehydedehydrogenase (ALDH). BODIPY aminoacetaldehydeconsists of an aminoacetaldehyde moiety bonded to

22、the BODIPY fluorochrome and can be used to labelstem cells.Purity: 98.87%Clinical Data: No Development ReportedSize: 1 gPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/cm037.html CM037(A37) Cat

23、. No.: HY-110294 HYPERLINK https:/www.MedChemE/cm10.html CM10Cat. No.: HY-135841CM037 is a selective inhibitor of ALDH1A1(aldehyde dehydrogenase 1A1) with an IC of 4.650M.CM10 is a potent and selective aldehydedehydrogenase 1A (ALDH1A) family inhibitor,with IC s of 1700, 740, and 640 nM for ALDH1A1,

24、50ALDH1A2, and ALDH1A3, respectively. CM10 does notinhibit any of the other ALDH family members.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.53%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cm121

25、.html CM121 HYPERLINK https:/www.MedChemE/cm121.html HYPERLINK https:/www.MedChemE/cvt-10216.html CVT-10216Cat. No.: HY-139032 Cat. No.: HY-19801CM121 is an active site-directed reversibleALDH1A2 inhibitor (IC =0.54 M =1.1 M)50 Kdwith a variety of hydrophobic interactions.CVT-10216 is a highly selec

26、tive, reversiblealdehyde dehydrogenase-2 (ALDH-2) inhibitor withan IC of 29 nM. CVT-10216 also has inhibitory50effect of ALDH-1 with an IC of 1.3 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25

27、mg, 50 mg HYPERLINK https:/www.MedChemE/disulfiram.html Disulfiram(Tetraethylthiuram disulfide; TETD) Cat. No.: HY-B0240 HYPERLINK https:/www.MedChemE/en40.html EN40Cat. No.: HY-122577Disulfiram (Tetraethylthiuram disulfide) is aspecific inhibitor of aldehyde-dehydrogenase(ALDH1), used for the treat

28、ment of chronicalcoholism by producing an acute sensitivity toalcohol.EN40 is a potent, selective aldehyde dehydrogenase3A1 (ALDH3A1) inhibitor as a covalent ligand,exhibits an IC value of 2 uM.50Purity: 99.77%Clinical Data: LaunchedSize: 10 mM 1 mL, 500 mg, 1 g, 5 gPurity: 95.15%Clinical Data: No D

29、evelopment ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ks106.html KS106 HYPERLINK https:/www.MedChemE/ks106.html HYPERLINK https:/www.MedChemE/medtc.html MeDTCCat. No.: HY-146683(S-Methyl-N,N-diethylthiocarbamate Sulfone) Cat. No.: HY-115757KS106 is a potent ALDH in

30、hibitor with IC s of50334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1,respectively. KS106 shows antiproliferative andanticancer effects with low low toxic.MeDTC (S-Methyl-N,N-diethylthiocarbamate Sulfone),a Disulfiram metabolite, is a potent, irreversiblealdehyde dehydrogenase (ALDH) inhibitor.Pur

31、ity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/NCT-501.html NCT-501 HYPERLINK https:/www.MedChemE/NCT-501.html HYPERLINK https:/www.MedChemE/nct-501-hydrochloride.html NCT-501 HYPERLINK https:/ww

32、w.MedChemE/nct-501-hydrochloride.html HYPERLINK https:/www.MedChemE/nct-501-hydrochloride.html hydrochlorideCat. No.: HY-18768 Cat. No.: HY-18768ANCT-501 is a potent and selectivetheophylline-based inhibitor of aldehydedehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1with IC of 40 nM, typically shows b

33、etter50selectivity over other ALDH isozymes and otherdehydrogenases (hALDH1B1, hALDH3A1, andNCT-501 hydrochloride is a potent and selectivetheophylline-based inhibitor of aldehydedehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1with IC of 40 nM, typically shows better50selectivity over other ALDH isozy

34、mes and otherdehydrogenases (hALDH1B1, hALDH3A1, andPurity: 99.84%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/NCT-505.html NCT-505 HYPERLINK https:/www.

35、MedChemE/NCT-505.html HYPERLINK https:/www.MedChemE/NCT-506.html NCT-506Cat. No.: HY-112277 Cat. No.: HY-112278NCT-505 is a potent and selective aldehydedehydrogenase (ALDH1A1) inhibitor, with an IC50of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3,hALDH2, hALDH3A1 (IC s, 57, 22.8, 20.1,5057 M).NCT-5

36、06 is an orally bioavailable aldehydedehydrogenase 1A1 (ALDH1A1) inhibitors with anIC of 7 nM.50Purity: 98.41%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/nitrefazo

37、le.html Nitrefazole(EMD-15700) Cat. No.: HY-107030 HYPERLINK https:/www.MedChemE/prunetin.html PrunetinCat. No.: HY-N2597Nitrefazole is a 4-nitroimidazole derivative withstrong and long lasting inhibition of aldehydedehydrogenase (ALDH), an enzyme involved in themetabolism of alcohol.Prunetin, an O-

38、methylated isoflavone, possessesanti-inflammatory activity. Prunetin is a potenthuman aldehyde dehydrogenases inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.01%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/rv01.html

39、 RV01 HYPERLINK https:/www.MedChemE/rv01.html HYPERLINK https:/www.MedChemE/taraxerone.html TaraxeroneCat. No.: HY-126241 Cat. No.: HY-N1177RV01 is an analogue of resveratrol, inhibits DNAdamage, reduces acetaldehyde dehydrogenase 2(ALDH2) mRNA expression induced by ethanol, andexhibits hydroxyl radical scavenging activity.RV01 decreases iNOS expression, withanti-neuroinflammator