β-catenin-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/-catenin.html -cateninBeta catenin-catenin is a dual function protein, regulating the coordination of cellcell adhesion and gene transcription. In humans, theCTNNB1 protein is encoded by the CTNNB1 gene. -catenin is a subunit of the cadherin protein complex and

2、 acts as anintracellular signal transducer in the Wnt signaling pathway. It is a member of the catenin protein family and homologous to-catenin. Mutations and overexpression of -catenin are associated with many cancers, including hepatocellular carcinoma,colorectal carcinoma, lung cancer,malignant b

3、reast tumors, ovarian and endometrial cancer. -catenin is regulated and destroyedby the beta-catenin destruction complex, and in particular by the adenomatous polyposis coli (APC) protein, encoded by thetumour-suppressing APC gene. Therefore genetic mutation of the APC gene is also strongly linked t

4、o cancers, and in particularcolorectal cancer resulting from familial adenomatous polyposis (FAP).www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/-catenin.html -catenin HYPERLINK https:/www.MedChemE/Targets/-catenin.html HYPERLINK https:/www.MedChemE/Targets/-catenin.html Inhibitors, HYPERLINK

5、https:/www.MedChemE/Targets/-catenin.html HYPERLINK https:/www.MedChemE/Targets/-catenin.html Agonists, HYPERLINK https:/www.MedChemE/Targets/-catenin.html HYPERLINK https:/www.MedChemE/Targets/-catenin.html Antagonists HYPERLINK https:/www.MedChemE/Targets/-catenin.html HYPERLINK https:/www.MedChem

6、E/Targets/-catenin.html & HYPERLINK https:/www.MedChemE/Targets/-catenin.html HYPERLINK https:/www.MedChemE/Targets/-catenin.html Activators HYPERLINK https:/www.MedChemE/e-ferulic-acid.html (E)-Ferulic HYPERLINK https:/www.MedChemE/e-ferulic-acid.html HYPERLINK https:/www.MedChemE/e-ferulic-acid.ht

7、ml acid(E)-Coniferic acid) Cat. No.: HY-N0060B HYPERLINK https:/www.MedChemE/e-ferulic-acid-d3.html (E)-Ferulic HYPERLINK https:/www.MedChemE/e-ferulic-acid-d3.html HYPERLINK https:/www.MedChemE/e-ferulic-acid-d3.html acid-d3(E)-Coniferic acid-d3) Cat. No.: HY-N0060BS(E)-Ferulic acid is a isomer of

8、Ferulic acid whichis an aromatic compound, abundant in plant cellwalls.(E)-Ferulic acid-d3 (E)-Coniferic acid-d3) is thedeuterium labeled (E)-Ferulic acid. (E)-Ferulicacid is a isomer of Ferulic acid which is anaromatic compound, abundant in plant cell walls.Purity: 99.20%Clinical Data: No Developme

9、nt ReportedSize: 10 mM 1 mL, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Astragaloside-I.html Astragaloside HYPERLINK https:/www.MedChemE/Astragaloside-I.html HYPERLINK https:/www.MedChemE/Astragaloside-I.html I(Astrasieversianin IV; Cyclosie

10、versioside B) Cat. No.: HY-N0432 HYPERLINK https:/www.MedChemE/cardiogenol-c.html Cardiogenol HYPERLINK https:/www.MedChemE/cardiogenol-c.html HYPERLINK https:/www.MedChemE/cardiogenol-c.html CCat. No.: HY-12319Astragaloside I, one of the main activeingredients in Astragalus membranaceus, hasosteoge

11、nic properties. Astragaloside I stimulatesosteoblast differentiation through theWnt/-catenin signaling pathway.Cardiogenol C is a potent cell-permeablepyrimidine inducer which prompts thedifferentiation of ESCs into cardiomyocytes(EC =100 nM).50Purity: 98.0%Clinical Data: No Development ReportedSize

12、: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Cardiogenol-C-hydrochloride.html Cardiogenol HYPERLINK https:/www.MedChemE/Cardiogenol-C-hydrochloride.html HYPERLINK https:/www.MedChemE/Cardiogenol-C-hydrochlorid

13、e.html C HYPERLINK https:/www.MedChemE/Cardiogenol-C-hydrochloride.html HYPERLINK https:/www.MedChemE/Cardiogenol-C-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Cardiogenol-C-hydrochloride.html HYPERLINK https:/www.MedChemE/cct031374-hydrobromide.html CCT031374 HYPERLINK https:/www

14、.MedChemE/cct031374-hydrobromide.html HYPERLINK https:/www.MedChemE/cct031374-hydrobromide.html hydrobromideCat. No.: HY-12319A Cat. No.: HY-108441Cardiogenol C hydrochloride is a potentcell-permeable pyrimidine inducer which promptsthe differentiation of ESCs into cardiomyocytes(EC =100 nM).50CCT 0

15、31374 hydrobromid is a potent inhibitor of-catenin/transcription factor (TCF) complexsignaling. CCT031374 inhibits TCF-dependenttranscription of genes of Wnt signaling pathway.CCT 031374 has antitumor activity.Purity: 99.76%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg,

16、50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cwp232228.html CWP232228 HYPERLINK https:/www.MedChemE/cwp232228.html HYPERLINK https:/www.MedChemE/dk419.html DK419Cat. No.: HY-18959 Cat. No.: HY-112799CWP232228, a highly potent selectiveW

17、nt/-catenin signaling inhibitor, antagonizesbinding of -catenin to T-cell factor (TCF) in thenucleus.DK419 is a potent and orally activeWnt/-catenin signaling inhibitor, with an IC50of 0.19 M. DK419 reduces protein lelvels ofAxin2, -catenin, c-Myc, Cyclin D1 and Survivinand induces production of pAM

18、PK.Purity: 98.31%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.68%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/fh535.html FH535 HYPERLINK https:/www.MedChemE/fh535.html HYPERLINK https:/www.MedChemE

19、/fzm1.html FzM1Cat. No.: HY-15721 Cat. No.: HY-116553FH535 is an inhibitor of Wnt/-catenin andPPAR, with anti-tumor activities.FzM1 is a negative allosteric modulator (NAM) ofFrizzled receptor FZD4. FzM1 reducesWNT5A-dependent WNT responsive element (WRE)activity (log EC =6.2).50inhPurity: 99.87%Cli

20、nical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/fzm1-8.html FzM1.8 HYPERLINK https:/www.MedChemE/fzm1-8.html HYPERLINK ht

21、tps:/www.MedChemE/ICG-001.html ICG-001Cat. No.: HY-117163 Cat. No.: HY-14428FzM1.8 derives from FzM1, is an allosteric agonistof FZD4 with pEC of 6.4. FzM1.8 binds to FZD450and activates the WNT/-catenin pathway, bypromoting TCF/LEF transcriptional activity in theabsence of any WNT ligand.ICG-001 is

22、 an inhibitor of -catenin/TCF mediatedtranscription. ICG-001 works by specificallybinding to cyclic AMP response element-bindingprotein with an IC of 3 M. ICG-001 selectively50blocks the -catenin/CBP interaction withoutinterfering with the -catenin/p300 interaction.Purity: 98.20%Clinical Data:Size:

23、10 mM 1 mL, 10 mg, 25 mg, 50 mgPurity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/icrt-5.html iCRT-5 HYPERLINK https:/www.MedChemE/icrt-5.html HYPERLINK https:/www.MedChemE/KY1220.html KY1220Cat. No.: HY-119383 Cat. No.: HY-

24、102028iCRT-5 is a -catenin-regulated transcription(CRT) inhibitor. iCRT-5 can blockWnt/-catenin reporter activity and downregulate -catenin expression. iCRT-5 can be usedfor the research of multiple myeloma.KY1220 is a compound that destabilizes both-catenin and Ras, via targeting theWnt/-catenin pa

25、thway; with an IC of 2.1 M50in HEK293 reporter cells.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ky19382.html KY19382(A3051) Cat. No.: HY-13

26、1447 HYPERLINK https:/www.MedChemE/KYA1797K.html KYA1797KCat. No.: HY-101090KY19382 is a potent and orally active dualinhibitor of CXXC5-DVL and GSK3, with IC s of5019 and 10 nM, respectively. KY19382 activatesWnt/-catenin signaling through inhibitory effectson both CXXC5-DVL interaction and GSK3 ac

27、tivity.KYA1797K is a potent and selectiveWnt/-catenin inhibitor with an IC of 0.7550M.Purity: 98.04%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www

28、.MedChemE/l-quebrachitol.html L-Quebrachitol HYPERLINK https:/www.MedChemE/l-quebrachitol.html HYPERLINK https:/www.MedChemE/CHIR-99021.html LaduviglusibCat. No.: HY-N2375(CHIR-99021; CT99021) Cat. No.: HY-10182L-Quebrachitol is a natural product isolated frommany plants, promotes osteoblastogenesis

29、 byuppregulation of BMP-2, runt-relatedtranscription factor-2 (Runx2), MAPK (ERK,JNK, p38), and Wnt/-catenin signalingpathway.Laduviglusib (CHIR-99021) is a potent andselective GSK-3/ inhibitor with IC s of 10 nM50and 6.7 nM. Laduviglusib shows 500-foldselectivity for GSK-3 over CDC2, ERK2 and other

30、protein kinases.Purity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 99.76%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/CHIR-99021-monohydrochloride.html Laduviglusib HYPERLINK https:/www.MedChemE/CHIR-

31、99021-monohydrochloride.html HYPERLINK https:/www.MedChemE/CHIR-99021-monohydrochloride.html monohydrochloride HYPERLINK https:/www.MedChemE/CHIR-99021-monohydrochloride.html HYPERLINK https:/www.MedChemE/CHIR-99021-trihydrochloride.html Laduviglusib HYPERLINK https:/www.MedChemE/CHIR-99021-trihydro

32、chloride.html HYPERLINK https:/www.MedChemE/CHIR-99021-trihydrochloride.html trihydrochloride(CHIR-99021 monohydrochloride; CT99021 monohydrochloridCea)t. No.: HY-10182A (CHIR-99021 trihydrochloride; CT99021 trihydrochloride) Cat. No.: HY-10182BLaduviglusib (CHIR-99021) monohydrochloride is apotent

33、and selective GSK-3/ inhibitor withIC s of 10 nM and 6.7 nM. Laduviglusib50monohydrochloride shows 500-fold selectivityfor GSK-3 over CDC2, ERK2 and other proteinkinases.Laduviglusib (CHIR-99021) trihydrochloride is apotent and selective GSK-3/ inhibitor withIC s of 10 nM and 6.7 nM. Laduviglusib50t

34、rihydrochloride shows 500-fold selectivityfor GSK-3 over CDC2, ERK2 and other proteinkinases.Purity: 99.93%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.68%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgwww.MedChemE 3 HYPERLIN

35、K https:/www.MedChemE/LF3.html LF3 HYPERLINK https:/www.MedChemE/LF3.html HYPERLINK https:/www.MedChemE/msab.html MSABCat. No.: HY-101486 Cat. No.: HY-120697LF3 is an antagonist of the -Catenin/TCF4interaction with antitumor activity; has an ICof 1.65 M.50MSAB is a potent and selective inhibitor ofW

36、nt/-catenin signaling. MSAB binds to-catenin promoting its degradation, andspecifically downregulates Wnt/-catenin targetgenes. MSAB exhibits potent anti-tumor effectsselectively on Wnt-dependent cancer cells.Purity: 99.55%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 5

37、0 mg, 100 mgPurity: 99.77%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/n-3-methoxybenzyl-9z-12z-15z-octadecatrienamide.html N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide HYPERLINK https:/www.MedChemE/n-3-methoxybenzyl-9

38、z-12z-15z-octadecatrienamide.html HYPERLINK https:/www.MedChemE/n-desmethylnefopam.html N-DesmethylnefopamCat. No.: HY-N7702 Cat. No.: HY-133115N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide is a macamide isolated from Maca (Lepidiummeyenii Walp.N-Desmethylnefopam is the main metabolite ofNefop

39、am. N-Desmethylnefopam is a centrally-actingbut non-opioid analgesic agent, for the relief ofmoderate to severe pain. Nefopam targets -cateninprotein level in mesenchymal cells in-vitro andin-vivo.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No D

40、evelopment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/n-desmethylnefopam-d5-hydrochloride.html N-Desmethylnefopam HYPERLINK https:/www.MedChemE/n-desmethylnefopam-d5-hydrochloride.html HYPERLINK https:/www.MedChemE/n-desmethylnefopam-d5-hydrochloride.html D5 HYPERLINK https:/www.MedChemE

41、/n-desmethylnefopam-d5-hydrochloride.html HYPERLINK https:/www.MedChemE/n-desmethylnefopam-d5-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/n-desmethylnefopam-d5-hydrochloride.html HYPERLINK https:/www.MedChemE/nefopam-d3-hydrochloride.html Nefopam HYPERLINK https:/www.MedChemE/nefo

42、pam-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/nefopam-d3-hydrochloride.html D3 HYPERLINK https:/www.MedChemE/nefopam-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/nefopam-d3-hydrochloride.html hydrochlorideCat. No.: HY-133115AS Cat. No.: HY-B1057SN-Desmethylnefopam D5 hydrochloride i

43、s a deuteriumlabeled N-Desmethylnefopam hydrochloride.N-Desmethylnefopam hydrochloride is the mainmetabolite of Nefopam.Nefopam D3 hydrochloride is the deuterium labeledNefopam hydrochloride. Nefopam hydrochloride(Fenazoxine hydrochloride) is a centrally-actingbut non-opioid analgesic drug, for the

44、relief ofmoderate to severe pain.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/Nefopam-hydrochloride.html Nefopam HYPERLINK https:/www.MedChemE/Nefopam-hydrochloride.html HYPERLINK http

45、s:/www.MedChemE/Nefopam-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Nefopam-hydrochloride.html HYPERLINK https:/www.MedChemE/nefopam-d3.html Nefopam-d3(Fenazoxine hydrochloride) Cat. No.: HY-B1057 (Fenazoxine-d3) Cat. No.: HY-B1057S2Nefopam hydrochloride (Fenazoxine hydrochloride)

46、is a centrally-acting but non-opioid analgesicdrug, for the relief of moderate to severe pain.Nefopam hydrochloride targets -catenin proteinlevel in mesenchymal cells in-vitro and in-vivo.Nefopam D3 (Fenazoxine D3) is a deuterium labeledNefopam (Fenazoxine). Nefopam is acentrally-acting but non-opio

47、id analgesic drug,and Nefopam targets -catenin protein level inmesenchymal cells.Purity: 99.78%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/nefopam-d4-hydrochloride.html Nefopam-d4 HYPERLINK https

48、:/www.MedChemE/nefopam-d4-hydrochloride.html HYPERLINK https:/www.MedChemE/nefopam-d4-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/nefopam-d4-hydrochloride.html HYPERLINK https:/www.MedChemE/nls-stax-h.html NLS-StAx-h(Fenazoxine-d4 hydrochloride) Cat. No.: HY-B1057S1Cat. No.: HY-P2

49、272Nefopam-d4 (hydrochloride) is deuterium labeledNefopam (hydrochloride). Nefopam hydrochloride(Fenazoxine hydrochloride) is a centrally-actingbut non-opioid analgesic drug, for the relief ofmoderate to severe pain.NLS-StAx-h is a selective, stapled peptideinhibitor of Wnt signaling with an IC of 1

50、.450M. NLS-StAx-h efficiently inhibits-catenin-transcription factor interactions.NLS-StAx-h inhibits proliferation and migration ofcolorectal cancer cells.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 100 g4 Tel: 609-228-6898

51、Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/nrx-103094.html NRX-103094 HYPERLINK https:/www.MedChemE/nrx-103094.html HYPERLINK https:/www.MedChemE/nrx-103095.html NRX-103095Cat. No.: HY-141449 Cat. No.: HY-141450NRX-103094 is a potent enhancer of the interactionbetween -cate

52、nin, and its cognate E3 ligase,SCF-TrCP. NRX-103094 enhances the binding ofpSer33/Ser37 -catenin peptide for -TrCP with anEC50 of 62 nM and a Kd of 0.6 nM.NRX-103095 is an enhancer of the interactionbetween -catenin, and its cognate E3 ligase,SCF-TrCP. NRX-103095 enhances the binding ofpSer33/Ser37

53、-catenin peptide for -TrCP with anEC of 163 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/nrx-252114.html NRX-252114 HYPERLINK https:/www.MedChemE/nrx-252114.html HYPERLINK https:/

54、www.MedChemE/NRX-252262.html NRX-252262Cat. No.: HY-111836 Cat. No.: HY-111760NRX-252114 is a potent enhancer of the interactionbetween -catenin, and its cognate E3 ligase,SCF-TrCP. NRX-252114 enhances the binding ofpSer33/S37A -catenin peptide for -TrCP with anEC50 of 6.5 nM and a Kd of 0.4 nM. NRX

55、-252114induces mutant -catenin degradation.NRX-252262 is a potent enhancer of the interactionbetween -Catenin, and its cognate E3 ligase,SCF-TrCP, induces mutant -catenin degradation,with an EC of 3.8 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.97%Clinical Data:

56、No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/nrx-2663.html NRX-2663 HYPERLINK https:/www.MedChemE/nrx-2663.html HYPERLINK https:/www.MedChemE/Pamidronic_acid.html Pamidronic HYPERLINK https:/www.MedChemE/Pamidronic_acid.html HYPERLINK https

57、:/www.MedChemE/Pamidronic_acid.html acidCat. No.: HY-141448 Cat. No.: HY-B0012NRX-2663 is an enhancer of the interaction between-catenin, and its cognate E3 ligase, SCF-TrCP.NRX-2663 enhances the binding of -catenin peptidefor -TrCP with an EC of 22.9 M and a of50 Kd54.8 nM.Pamidronic acid is a drug

58、 used to treat a broadspectrum of bone absorption diseases.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg HYPERLINK https:/www.MedChemE/PNU-74654.html PNU-74654 HYPERLINK https:/www.MedChemE/PNU-7465

59、4.html HYPERLINK https:/www.MedChemE/Salinomycin.html SalinomycinCat. No.: HY-101130(Procoxacin) Cat. No.: HY-15597PNU-74654 is an inhibitor of Wnt/-cateninpathway with an IC of 129.8 M in NCI-H295 cell.50Salinomycin (Procoxacin), a polyether potassiumionophore antibiotic, selectively inhibits thegr

60、owth of gram-positive bacteria. Salinomycin isa potent inhibitor of Wnt/-catenin signaling,blocks Wnt-induced LRP6 phosphorylation.Purity: 99.42%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1