Smo-Antagonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Smo.html SmoSmoothenedSmoothened (Smo), a class Frizzled G protein-coupled receptor (class F GPCR), transduces the Hedgehog (Hh) signal across the cellmembrane. The Hh signaling pathway includes both canonical and noncanonical pathways. The canonical Hh pathway

2、 functionsthrough major Hh molecules such as Hh ligands, PTCH, Smo, and GLI, whereas the noncanonical Hh pathway involves the activationof Smo or GLI through other pathways.The Hh signaling cascade is initiated by the binding of the Hh protein ligand to its cellular membrane receptor, Patched (PTCH)

3、,which relieves PTCH-mediated repression of the seven-transmembrane (7TM) protein Smo. Activated Smo transduces the signal tothe GLI family of transcription factors, which translocate to the nucleus to regulate numerous gene products involved in tissuepatterning and cell differentiation.www.MedChemE

4、 1 HYPERLINK https:/www.MedChemE/Targets/Smo.html Smo HYPERLINK https:/www.MedChemE/Targets/Smo.html HYPERLINK https:/www.MedChemE/Targets/Smo.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Smo.html HYPERLINK https:/www.MedChemE/Targets/Smo.html Agonists, HYPERLINK https:/www.MedChemE/Target

5、s/Smo.html HYPERLINK https:/www.MedChemE/Targets/Smo.html Antagonists HYPERLINK https:/www.MedChemE/Targets/Smo.html HYPERLINK https:/www.MedChemE/Targets/Smo.html & HYPERLINK https:/www.MedChemE/Targets/Smo.html HYPERLINK https:/www.MedChemE/Targets/Smo.html Activators HYPERLINK https:/www.MedChemE

6、/20-s-hydroxycholesterol.html 20(S)-Hydroxycholesterol(20-Hydroxycholesterol) Cat. No.: HY-12316 HYPERLINK https:/www.MedChemE/allo-2.html ALLO-2Cat. No.: HY-11740720(S)-hydroxyCholesterol (20-Hydroxycholesterol)is an allosteric activator of the oncoproteinsmoothened (Smo) that activates the hedgeho

7、g(Hh) signaling pathway with an EC of 3 M in a50gene transcription reporter assay using NIH3T3cells.ALLO-2 is a potent drug-resistant Smoothened(Smo) mutant antagonist that inhibits Smoagonist Hh-Ag1.5-induced luciferase expression inTM3-Gli-Luc cells with IC of 6 nM.50Purity: 98.07%Clinical Data: N

8、o Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 99.58%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bms-833923.html BMS-833923(XL-139) Cat. No.: HY-13809 HYPERLINK https:/www.MedChemE/cur61414.html CUR61414Cat. No.: HY-113

9、965BMS-833923 (XL-139) is an orally bioavailablesmall-molecule inhibitor of Smoothened withpotential antineoplastic activity; inhibits BODIPYcyclopamine binding to SMO in a dose-dependentmanner with an IC50 of 21 nM.Purity: 98.21%Clinical Data: Phase 2Size: 10 mM 1 mL, 10 mg, 50 mg, 100 mgCUR61414 i

10、s a novel, potent and cell permeableHedgehog signaling pathway inhibitor(IC =100-200 nM). CUR61414 is a50small-molecule aminoproline class compound andselectively binds to smoothened (Smo) with aK value of 44 nM.iPurity: 99.0%Clinical Data: No Development ReportedSize: 10 mg HYPERLINK https:/www.Med

11、ChemE/Cyclopamine.html Cyclopamine(11-Deoxojervine) Cat. No.: HY-17024 HYPERLINK https:/www.MedChemE/DY131.html DY131(GSK 9089) Cat. No.: HY-15483Cyclopamine is a Hedgehog (Hh) pathwayantagonist with an IC of 46 nM in the Hh cell50assay. Cyclopamine is also a selective Smoinhibitor.DY131 (GSK 9089)

12、is a potent and selective ERRand ERR agonist. DY131displays inactive againstERR, ER and ER. DY131 also inhibits Smosignaling.Purity: 99.97%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 1

13、00 mg HYPERLINK https:/www.MedChemE/PF-04449913.html Glasdegib HYPERLINK https:/www.MedChemE/PF-04449913.html HYPERLINK https:/www.MedChemE/gsa-10.html GSA-10(PF-04449913) Cat. No.: HY-16391Cat. No.: HY-12317Glasdegib (PF-04449913) is a potent and orallybioavailable smoothened inhibitor. Glasdegib(P

14、F-04449913) binds to human SMO (amino acids181-787) with an IC of 4 nM.50GSA-10 is a potent agonist of Smoothened (Smo)receptor with an EC of 1.2 M. GSA-10 is a50novel quinolinecarboxamide derivative. GSA-10 actsat Smo to promote the differentiation ofmultipotent mesenchymal progenitor cells intoost

15、eoblasts.Purity: 99.31%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Halcinonide.html Halcinonide HYPERLINK https:/www.MedChemE/Halcinonide.html HYPERLINK https:/www.MedChemE/HhAntag.html H

16、hAntag(SQ-18566) Cat. No.: HY-B0877Cat. No.: HY-15412Halcinonide (SQ-18566) is a high potencycorticosteroid used topically in the treatment ofcertain skin conditions.HhAntag is a specific, potent and orally activesmall molecule SMO antagonist of the Hhpathway.Purity: 99.87%Clinical Data: LaunchedSiz

17、e: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mgPurity: 98.70%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/ihr-1.html IHR-1 HYPERLINK https:/www.MedChemE/ihr-1.html HYPERLINK http

18、s:/www.MedChemE/ihr-cy3.html IHR-Cy3Cat. No.: HY-110240 Cat. No.: HY-131016IHR-1 is a cell membrane impermeable Smoantagonist.IHR-Cy3 is a potent fluorescent Smo antagonistwith an IC of 100 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development

19、 ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Jervine.html Jervine(11-Ketocyclopamine) Cat. No.: HY-N0836 HYPERLINK https:/www.MedChemE/kaad-cyclopamine.html KAAD-Cyclopamine(Cyclopamine-KAAD) Cat. No.: HY-100535Jervine (11-Ketocyclopamine) is a potent Hedgehog(Hh) inhibitor with an IC of

20、500-700 nM.50Jervine is a natural teratogenic sterodialalkaloid from rhizomes of Veratrum album.Jervine has anti-inflammatory and antioxidantproperties.KAAD-Cyclopamine, a hedgehog signaling inhibitor,is a smoothened antagonist.Purity: 99.03%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 5

21、0 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/LEQ506.html LEQ506(NVP-LEQ506) Cat. No.: HY-18636 HYPERLINK https:/www.MedChemE/MK-4101.html MK-4101Cat. No.: HY-100036LEQ506 is a second-generation inhibitor ofsmoothened (Smo) with IC s of 2

22、 and 4 nM in50human and mouse, respectively.MK-4101 is a Smoothened (SMO) antagonist(IC of 1.1 M for 293 cells ) and also a potent50inhibitor of the hedgehog pathway (IC of 1.550M for mouse cells; IC of 1 M for KYSE18050oesophageal cancer cells).Purity: 98.15%Clinical Data: No Development ReportedSi

23、ze: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.31%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/mrt-10.html MRT-10 HYPERLINK https:/www.MedChemE/mrt-10.html HYPERLINK https:/www.MedChemE/mrt-14.html MRT-14Cat. No.: HY-1

24、08507 Cat. No.: HY-145918MRT-10 is a seven-transmembrane receptorsmoothened (Smo) antagonist with an IC of500.65 M in the micromolar range in variousHedgehog (Hh) assays. MRT-10 binds to the Smoreceptor at the level of the Bodipycyclopaminebinding site.MRT-14 is a potent antagonist of Smo. Smo isthe

25、 major component involved in signaltransduction of the Hedgehog (Hh) morphogens.MRT-14 has the potential for the research ofseveral types of cancers linked to abnormal Hhsignaling.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clinical Data: No Development

26、 ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/mrt-81.html MRT-81 HYPERLINK https:/www.MedChemE/mrt-81.html HYPERLINK https:/www.MedChemE/MRT-83.html MRT-83Cat. No.: HY-145387 Cat. No.: HY-18287MRT-81 is a potent antagonist of human and rodentsmoothened (Smo) receptors, with an IC value50of

27、 41 nM in the Shh-light2 cells. MRT-81 haspotent hedgehog inhibiting activity. MRT-81 can beused for the research of cancer.MRT-83 is a potent antagonist of Smo, with anIC in the nanomolar range. MRT-83 also blocks50Hedgehog (Hh) signaling.Purity: 98.87%Clinical Data: No Development ReportedSize: 5

28、mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.16%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/mrt-83-hydrochloride.html MRT-83 HYPERLINK https:/www.MedChemE/mrt-83-hydrochloride.html HYPERLINK https:/www.MedChemE/mrt-83-hydroch

29、loride.html hydrochloride HYPERLINK https:/www.MedChemE/mrt-83-hydrochloride.html HYPERLINK https:/www.MedChemE/pf-5274857.html PF-5274857Cat. No.: HY-18287A Cat. No.: HY-13459MRT-83 (hydrochloride) is the potent antagonist ofSmoothened (Smo) receptor. MRT-83(hydrochloride) inhibits the Hedgehog (Hh

30、)signaling pathway and BODIPY-cyclopamine bindingto human Smo. MRT-83 (hydrochloride) has thepotential for researching cancer disease.PF-5274857 is a potent, selective, orally activeand brain-penetrant antagonist of Smo, with anIC of 5.8 nM and of 4.6 nM. PF-5274857 has50 Kipotential for research of

31、 tumor types includingbrain tumors and brain metastasis driven by anactivated Hh pathway.Purity: 99.60%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.12%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.Me

32、dChemE/pf-5274857-hydrochloride.html PF-5274857 HYPERLINK https:/www.MedChemE/pf-5274857-hydrochloride.html HYPERLINK https:/www.MedChemE/pf-5274857-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/pf-5274857-hydrochloride.html HYPERLINK https:/www.MedChemE/Purmorphamine.html Purmorpha

33、mineCat. No.: HY-13459A Cat. No.: HY-15108PF-5274857 hydrochloride is a potent, selective,orally active and brain-penetrant antagonist ofSmo IC50 Ki, with an of 5.8 nM and of 4.6 nM.Purmorphamine is a smoothened/Smo receptoragonist with an EC of 1 M.50Purity: 98%Clinical Data: No Development Reporte

34、dSize: 1 mg, 5 mgPurity: 99.89%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/SAG.html SAG HYPERLINK https:/www.MedChemE/SAG.html HYPERLINK https:/www.MedChemE/sag-dihydrochloride.html SAG HYPERLINK https:/www.MedChemE/sag-dihydrochloride.htm

35、l HYPERLINK https:/www.MedChemE/sag-dihydrochloride.html dihydrochlorideCat. No.: HY-12848 Cat. No.: HY-12848CSAG is a potent Smoothened (Smo) receptoragonist (EC50=3 nM; Kd=59 nM). SAG activatesthe Hedgehog signaling pathway and counteractsCyclopamine (HY-17024) inhibition of Smo.SAG dihydrochlorid

36、e is a potent Smoothened(Smo) receptor EC50 Kdagonist ( =3 nM; =59 nM).SAG dihydrochloride activates the Hedgehogsignaling pathway and counteracts Cyclopamine(HY-17024) inhibition of Smo.Purity: 99.88%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%C

37、linical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/SAG_hydrochloride.html SAG HYPERLINK https:/www.MedChemE/SAG_hydrochloride.html HYPERLINK https:/www.MedChemE/SAG_hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/SAG_hydrochlo

38、ride.html HYPERLINK https:/www.MedChemE/sag-d3.html SAG-d3Cat. No.: HY-12848B Cat. No.: HY-12848SSAG hydrochloride is a potent Smoothened (Smo)receptor agonist (EC =3 nM; =59 nM). SAG50 Kdhydrochloride activates the Hedgehog signalingpathway and counteracts Cyclopamine (HY-17024)inhibition of Smo.SA

39、G-d3 is deuterium labeled SAG. SAG is a potentSmoothened (Smo) receptor agonist (EC =350nM; K =59 nM).dPurity: 99.58%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98.77%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www

40、.MedChemE/saikosaponin-b1.html Saikosaponin HYPERLINK https:/www.MedChemE/saikosaponin-b1.html HYPERLINK https:/www.MedChemE/saikosaponin-b1.html B1 HYPERLINK https:/www.MedChemE/saikosaponin-b1.html HYPERLINK https:/www.MedChemE/SANT-1.html SANT-1Cat. No.: HY-N0247 Cat. No.: HY-100224Saikosaponin B

41、1 is a bioactive constituent of RadixBupleuri with anticancer activity. Saikosaponin B1significantly inhibits tumor growth inMedulloblastoma (MB) model by inhibiting theHedgehog pathway through targeting SMO.SANT-1, a potent Smo antagonist, inhibitsHedgehog signaling. SANT-1 shows IC s of 20 nM50and

42、 30 nM in Shh-LIGHT2 and SmoA1-LIGHT2 assay,respectively.Purity: 99.42%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.88%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 HYPERLINK https:/www.MedCh