BCC5441
RU-SKI 43
RU-SKI 43 is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 has anti-cancer activity.
BCC3935
LY2940680
Taladegib (LY2940680) is an antagonist of the smoothened receptor.
BCC3838
PF-5274857
PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.
BCC3939
Ciliobrevin A
Ciliobrevin A is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM.
BCC7136
U 18666A
U18666A, a cell permeable drug, is a cholesterol synthesis and transport inhibitor.
BCC3941
SANT-1
SANT-1, a potent Smo antagonist, inhibits Hedgehog signaling. SANT-1 shows IC50s of 20 nM and 30 nM in Shh-LIGHT2 and SmoA1-LIGHT2 assay, respectively.
BCC3936
JK 184
JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
BCC3940
AY 9944 dihydrochloride
AY 9944 is a specific cholesterol biosynthesis inhibitor. AY 9944 inhibits the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme (IC50=13 nM). AY 9944 causes hypocholesterolemia and accumulation of 7DHC. At high doses, AY 9944 inhibits also in cultured embryos sterol Δ7-Δ8 isomerase, which causes the accumulation of cholest-8-en-3β-ol.
BCN2964
Cyclopamine
Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay.
BCN2975
Jervine
Jervine (11-Ketocyclopamine) is a potent Hedgehog (Hh) inhibitor with an IC50 of 500-700 nM. Jervine is a natural teratogenic sterodial alkaloid from rhizomes of Veratrum album. Jervine has anti-inflammatory and antioxidant properties.
BCC1090
GANT61
GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.
BCC7937
20(S)-Hydroxycholesterol
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
BCC1285
GDC-0449 (Vismodegib)
Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. It also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively.
BCC6390
SAG
SAG is a potent Smo receptor agonist which activates the Hedgehog signaling pathway with a Kd of 59 nM.
