Hedgehog-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Hedgehog.html HedgehogHedgehog (Hh) is composed of N-terminal and C-terminal domains that dissociate in a self-catalyzed proteolytic cleavage reaction.The N-terminal product HhNp, modified by cholesterol during self-cleavage, harbors all known Hh signaling acti

2、vities. Whensynthesized in the absence of the C-terminal domain (and hence lacking cholesterol modification), the N-terminal domain isaberrantly targeted and released selectively into the retina.Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers

3、. Hh ligands bind to andsuppress the transmembrane receptor Patched (PTCH), which suppresses Smoothened (SMO), a seven-transmembrane-helixprotein that positively regulates the Hh pathway.Sonic hedgehog (Shh) is a morphogen essential to the developing nervous system that continues to play an importan

4、t role in adultlife by contributing to cell proliferation and differentiation, maintaining blood-brain barrier integrity, and being cytoprotectiveagainst oxidative and excitotoxic stress, all features of importance in amyotrophic lateral sclerosis (ALS).Indian hedgehog (Ihh), a signaling molecule th

5、at plays a pivotal role in the regulation of chondrocyte proliferation, maturation, andossification both in long-bone development and digit joint formation, has also been found to be essential for temporomandibularjoint (TMJ) development.Desert hedgehog (Dhh), one of the Hedgehog family members, is

6、expressed by Schwann cells of peripheral nerves.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Hedgehog.html Hedgehog HYPERLINK https:/www.MedChemE/Targets/Hedgehog.html HYPERLINK https:/www.MedChemE/Targets/Hedgehog.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Hedgehog.html HYPERLIN

7、K https:/www.MedChemE/Targets/Hedgehog.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Hedgehog.html HYPERLINK https:/www.MedChemE/Targets/Hedgehog.html Antagonists HYPERLINK https:/www.MedChemE/Targets/Hedgehog.html HYPERLINK https:/www.MedChemE/Targets/Hedgehog.html & HYPERLINK https:/www.Med

8、ChemE/Targets/Hedgehog.html HYPERLINK https:/www.MedChemE/Targets/Hedgehog.html Activators HYPERLINK https:/www.MedChemE/Ciliobrevin-A.html Ciliobrevin HYPERLINK https:/www.MedChemE/Ciliobrevin-A.html HYPERLINK https:/www.MedChemE/Ciliobrevin-A.html A(HPI-4) Cat. No.: HY-100790 HYPERLINK https:/www.

9、MedChemE/ciliobrevin-d.html Ciliobrevin HYPERLINK https:/www.MedChemE/ciliobrevin-d.html HYPERLINK https:/www.MedChemE/ciliobrevin-d.html DCat. No.: HY-122632Ciliobrevin A (HPI-4) is a hedgehog (Hh)signaling pathway inhibitor with median inhibitoryconcentration (IC ) less than 10 M.50Ciliobrevin D i

10、s a cell-permeable, reversible andspecific inhibitor of AAA+ ATPase motorcytoplasmic dynein. Ciliobrevin D inhibitsHedgehog (Hh) signaling and primary ciliaformation. Ciliobrevin D inhibits dynein-dependentmicrotubule gliding and ATPase activity in vitro.Purity: 98.72%Clinical Data: No Development R

11、eportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.94%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/cur61414.html CUR61414Cat. No.: HY-113965 HYPERLINK https:/www.MedChemE/Cyclopamine.html Cyclopamine(11-Deoxojervine

12、) Cat. No.: HY-17024CUR61414 is 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:

13、10 mgCyclopamine is a Hedgehog (Hh) pathwayantagonist with an IC of 46 nM in the Hh cell50assay. Cyclopamine is also a selective Smoinhibitor.Purity: 99.97%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/dynarrestin.html DynarrestinCat. No.: HY-12

14、1802 HYPERLINK https:/www.MedChemE/hh-ag1-5.html Hh-Ag1.5(SAg1.5) Cat. No.: HY-124899Dynarrestin is a aminothiazole inhibitor ofcytoplasmic dyneins 1 and 2.Hh-Ag1.5 (SAg1.5) is a potent Hedgehog (Hh)agonist with an EC of 1 nM. Hh-Ag1.5 mediated50reprogramming breaks the quiescence of noninjuredliver

15、 stem cells for rescuing liver failure.Purity: 98.40%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mgPurity: 99.97%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Itraconazole.html Itraconazole HYPERLINK https:/www.MedChemE/It

16、raconazole.html HYPERLINK https:/www.MedChemE/itraconazole-d5.html Itraconazole-d5(R51211) Cat. No.: HY-17514Cat. No.: HY-17514SItraconazole (R51211) is a triazole antifungalagent and a potent and orally active Hedgehog(Hh) signaling pathway antagonist with an IC50of 800 nM.Itraconazole-d5 (R51211-d

17、5) is the deuteriumlabeled Itraconazole. Itraconazole (R51211) is atriazole antifungal agent and a potent and orallyactive Hedgehog (Hh) signaling pathwayantagonist with an IC of 800 nM.50Purity: 99.15%Clinical Data: LaunchedSize: 100 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize:

18、500 g, 1 mg HYPERLINK https:/www.MedChemE/Jervine.html Jervine HYPERLINK https:/www.MedChemE/Jervine.html HYPERLINK https:/www.MedChemE/JK184.html JK184(11-Ketocyclopamine) Cat. No.: HY-N0836Cat. No.: HY-13307Jervine (11-Ketocyclopamine) is a potent Hedgehog(Hh) inhibitor with an IC of 500-700 nM.50

19、Jervine is a natural teratogenic sterodialalkaloid from rhizomes of Veratrum album.Jervine has anti-inflammatory and antioxidantproperties.JK184 is a potent Hedgehog (Hh) pathwayinhibitor with IC of 30 nM in mammalian cells.50Purity: 99.03%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50

20、mg, 100 mgPurity: 99.37%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/MK-4101.html MK-4101 HYPERLINK https:/www.MedChemE/MK-4101.html HYPERLINK https:/www.MedChemE/neurodazine

21、.html NeurodazineCat. No.: HY-100036 Cat. No.: HY-108439MK-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).Neurodazine is an imidazole-based small mo

22、lecule,serve as a promoter of neurogenesisin pluripotentcells. Neurodazine promotes neurogenesis byactivating Wnt and Shh signaling pathways.Neurodazine selectively suppresses astrocytedifferentiation of P19 cells.Purity: 98.31%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 m

23、g, 25 mg, 50 mg, 100 mgPurity: 98.21%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/robotnikinin.html Robotnikinin HYPERLINK https:/www.MedChemE/robotnikinin.html HYPERLINK https:/www.MedChemE/ru-ski-43.html RU-SKI HYPERLINK https:/www.MedChemE/ru-s

24、ki-43.html HYPERLINK https:/www.MedChemE/ru-ski-43.html 43Cat. No.: HY-100515 Cat. No.: HY-18366Robotnikinin is a small molecule capable ofbinding to and inhibiting the activity of SonicHedgehog (Shh) signaling up stream of Smo.RU-SKI 43 is a potent and selective Hedgehogacyltransferase (Hhat) inhib

25、itor with an IC of50850 nM. RU-SKI 43 reduces Gli-1 activation throughSmoothened-independent non-canonical signaling anddecreases Akt and mTOR pathway activity. RU-SKI 43has anti-cancer activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development

26、 ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/RU-SKI-43-hydrochloride.html RU-SKI HYPERLINK https:/www.MedChemE/RU-SKI-43-hydrochloride.html HYPERLINK https:/www.MedChemE/RU-SKI-43-hydrochloride.html 43 HYPERLINK https:/www.MedChemE/RU-SKI-43-hydrochloride.html HYPERLINK https:/www.MedChem

27、E/RU-SKI-43-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/RU-SKI-43-hydrochloride.html HYPERLINK https:/www.MedChemE/sant-2.html SANT HYPERLINK https:/www.MedChemE/sant-2.html HYPERLINK https:/www.MedChemE/sant-2.html 2Cat. No.: HY-18366A Cat. No.: HY-107408RU-SKI 43 hydrochloride i

28、s a potent and selectiveHedgehog acyltransferase (Hhat) inhibitor withan IC of 850 nM. RU-SKI 43 hydrochloride reduces50Gli-1 activation through Smoothened-independentnon-canonical signaling and decreases Akt and mTORpathway activity.SANT 2 is a potent antagonist of Hh-signalingpathway. Hedgehog (Hh) signaling plays animportant role