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You are here:Home-Inhibitors & Agonists-Wnt/Notch/Hedgehog-Hedgehog (Hh)

Request The Product List ofHedgehog (Hh) Hedgehog (Hh)

Hedgehog (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 activities. When synthesized in the absence of the C-terminal domain (and hence lacking cholesterol modification), the N-terminal domain is aberrantly targeted and released selectively into the retina.

Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers. Hh ligands bind to and suppress the transmembrane receptor Patched (PTCH), which suppresses Smoothened (SMO), a seven-transmembrane-helix protein that positively regulates the Hh pathway.

Sonic hedgehog (Shh) is a morphogen essential to the developing nervous system that continues to play an important role in adult life by contributing to cell proliferation and differentiation, maintaining blood-brain barrier integrity, and being cytoprotective against oxidative and excitotoxic stress, all features of importance in amyotrophic lateral sclerosis (ALS).

Indian hedgehog (Ihh), a signaling molecule that plays a pivotal role in the regulation of chondrocyte proliferation, maturation, and ossification both in long-bone development and digit joint formation, has also been found to be essential for temporomandibular joint (TMJ) development.

Desert hedgehog (Dhh), one of the Hedgehog family members, is expressed by Schwann cells of peripheral nerves.

Cat. No. Product Name CAS No. Information
GY02101

RU-SKI 43

1043797-53-0

A small molecule inhibitor of Hhat (Hedgehog acyltransferase) with IC50 of 0.85 uM; specific to Shh palmitoylation and no effect for palmitoylation of H-Ras, Fyn and myristoylation of c-Src; reduces pancreatic cancer cell proliferation and Gli-1 activation through Smoothened-independent non-canonical signaling, inhibits two key proliferative pathways regulated by Akt and mTOR.

GY02020

RU-SKI 43 hydrochloride

1782573-67-4

A small molecule inhibitor of Hhat (Hedgehog acyltransferase) with IC50 of 0.85 uM; specific to Shh palmitoylation and no effect for palmitoylation of H-Ras, Fyn and myristoylation of c-Src; reduces pancreatic cancer cell proliferation and Gli-1 activation through Smoothened-independent non-canonical signaling, inhibits two key proliferative pathways regulated by Akt and mTOR.

GY03145

Ciliobrevin A

302803-72-1

Ciliobrevin A is a small molecule Hedgehog pathway inhibitor (IC50=7 uM) that acts downstream of Su(fu) to modulate Gli processing, activation or trafficking; does not directly target Smo, blocks the proliferation of cerebellar granule neuron precursors expressing an oncogenic form of Smo; disrupts spindle pole assembly and kinetochore-microtubule attachment, inhibits melanosome aggregation and peroxisome motility in cultured cells; inhibits AAA+ ATPase motor cytoplasmic dynein.

GY06432

Robotnikinin

1132653-79-2

Robotnikinin is asmall molecule that binds the extracellular Sonic Hedgehog (Shh) protein (Kd=3.1 uM) and blocks Shh-signaling in cell lines, human primary keratinocytes and synthetic model of human skin; displays significant repression of Shh-induced Gli1/Gli2, and interferes with the ability of the ShhN protein complex to relay its signal efficiently to Ptc1.

GY06426

Cyclopamine tartrate

1178510-81-0

Cyclopamine tartrate is a natural steroidal alkaloid that inhibits hedgehog (Hh) signaling with IC50 of 46 nM; inhibits hedgehog-dependent expression of Pax7 with IC50 of 24 nM, blocks the response of neural plate explants to recombinant Shh-N; A useful tool in studying the role of Hh in normal development, and as a potential treatment for certain cancers in which Hh is overexpressed.

GY06423

TAK-441

1186231-83-3

TAK-441 (TAK 441;TAK441) is a highly potent, orally active hedgehog signaling (Hh) inhibitor with IC50 of 4.4 nM in Gli-luc reporter assays; suppresses transcription factor Gli1 mRNA expression in tumor-associated stromal tissue and inhibits tumor growth in mouse medulloblastoma allograft model.

GY06422

GLPG-0492

1215085-92-9

GLPG-0492 (GLPG0492) is a novel, orally active, non-steroidal selective androgen receptor modulator (SARM) with in vitro potency of 13 nM; exhibits anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate in a classical model of orchidectomized rat; shows a potential treatment for Duchenne muscular dystrophy (DMD).

GY06419

BRD50837

1314295-24-3

BRD50837(BRD 50837) is a potent, selective, small-molecule inhibitor of the Sonic Hedgehog (Shh) pathway with EC50 of 90 nM, partially lowers Gli1 expression at concentrations of 2 uM, a useful probe of Shh signaling pathway.

GY06415

BRD9526

1446352-30-2

BRD9526(BRD 9526) is a potent, small-molecule inhibitor of the Sonic Hedgehog (Shh) pathway with EC50 of 60 nM, partially lowers Gli1 expression at concentrations of 10 uM, a useful probe of Shh signaling pathway.

GY06411

RUSKI-201

1458031-48-5

RUSKI-201 (RUSKI 201;RUSKI201) is a potent, selective and cell active Hedgehog acyltransferase (Hhat) inhibitor with IC50 of 0.87 uM; blocks Hh signaling in H520, Panc-1, and MCF-7 coculture with Shh-Light2 cells (IC50=4.8 uM, 7.8 uM, and 8.5 uM, respectively); selectively inhibits Hh palmitoylation over a panel of >100 palmitoylated substrates in cells.

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