Rhonin is a first small-molecule ligand of the RHO GDP-dissociation inhibitor 1 (RHOGDI1), binds to RHOGDI (Ki=2.2 uM), is an inhibitor of Hh-induced osteogenesis.Rhonin interferes with its function by disrupting the interaction between RHOGDI and RHO GTPases.Rhonin alters the subcellular localization of RHO GTPases.Rhonin inhibited RHOGDI1-mediated extraction of RAC1 from liposomes, Rhonin increased the levels of GTP-bound RHO GTPases, did not alter the total levels of the three RHO GTPasesRhonin an inhibitor of Hh-induced osteogenesis, but does not efficiently target canonical Hh signaling and SMO, directly targets RHOGDI, impairs RHOGDI function.

Picoberin is a highly potent (low picomolar) inhibitor of purmorphamine- and Sonic Hedgehog (Shh)-induced osteogenesis with IC50 of 3 pM, acts as an AhR agonist and induces the expression of AhR target genes, thereby suppressing osteoblast differentiation

MDB5 is a potent hedgehog (Hh) signaling pathway inhibitor, exhibits stronger inhibition of the Hh pathway and anticancer effect in vitro and vivo than GDC-0449.

Cyclopamine(11-Deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM.

RL-0070933 is a potent smo cilial modulator with an EC50 value of 0.02 µM. RL-0070933 modulates the translocation and/or accumulation of smoothened to the primary cilia by hedgehog signaling pathway.

RUSKI-201 dihydrochloride is a potent and specific Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 0.20 μM. RUSKI-201 dihydrochloride is able to block Hh signaling from Shh overexpressing cells and inhibits Hh palmitoylation. RUSKI-201 dihydrochloride is potential Hhat chemical probe in cells and can used in studies of Hhat catalytic function.

3-epi-Vitamin D3 (Epicholecalciferol) (Compound 4), a Vitamin D3 analogue, is a Hedgehog pathway inhibitor with an IC50 of 39.2 μM measured in U87MG cells.

SANT 2 is a potent antagonist of Hh-signaling pathway. Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. SANT 2 has the potential for the research of several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers.

Ciliobrevin A(HPI-4) is a Hedgehog pathway inhibitor and ciliogenesis inhibitor.

A small molecule inhibitor of Hhat (Hedgehog acyltransferase) with IC50 of 0.85 uM.

RU-SKI 43 Hcl is a small molecule inhibitor of Hhat(Hedgehog acyltransferase), the enzyme responsible for the attachment of palmitate onto Shh.

A highly potent, orally active hedgehog signaling (Hh) inhibitor with IC50 of 4.4 nM in Gli-luc reporter assays.