hedgehog inhibitor

RU-SKI 43 is a potent and selective hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. It exhibits anticancer activity and is a potential treatment for lung adenocarcinomas. RU-SKI 43 reduces Gli-1 activation through smoothening-independent non-canonical signaling and inhibits Akt and mTOR pathway activity.

CUR61414 is a cell-permeable inhibitor of Hedgehog signaling pathway (IC50 =100-200 nM) and selectively binds to smoothened (Ki = 44 nM).

CUR61414 hydrochloride is a potent and cell permeable inhibitor of Hedgehog signaling pathway (IC50 =100-200 nM). CUR61414 hydrochloride is a small-molecule aminoproline class compound. CUR61414 hydrochloride selectively binds to smoothened (Smo, Ki= 44 nM). CUR61414 hydrochloride can induce cancer cells apoptosis without affecting neighboring non-tumor cells.

LGE-899 (Sonidegib metabolite M48) is a main metabolite of Sonidegib which is an inhibitor of the hedgehog pathway. The Tmax of LGE-899(60 h) is much longer than Sonidegib.

Triparanol (NSC-65345) interferes with posttranslational modification of Hedgehog signaling molecules as well as the sterol sensing domain of its receptor PTCH1, leading to down-regulation of Hedgehog signaling. Triparanol suppresses human tumor growth and is an antilipemic agent with high ophthalmic toxicity.

Ellagic acid (Gallogen), a thickened tetracyclic natural product, is a potent CK2 inhibitor (IC50=40 nM; Ki=20 nM) with ATP-competitive properties. Ellagic acid is an antioxidant and also possesses antiproliferative activity.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

Tolnaftate (NP-27) is a synthetic antifungal agent used to treat skin infections caused by fungi.

Mebendazole (Mebenvet) is a hedgehog inhibitor, used as an antihelminthic.

Naftifine Hydrochloride is the hydrochloride salt form of naftifine, an allylamine derivate with synthetic broad-spectrum antifungal activity. Although the exact mechanism through which naftifine hydrochloride exerts its effect is unknown, it appears to selectively inhibit the enzyme squalene 2, 3-epoxidase, thereby inhibiting the biosynthesis of sterol. This results in a decreased amount of sterols, especially ergosterol which is the primary fungal membrane sterol, and a corresponding accumulation of squalene in fungal cells. Naftifine hydrochloride (Naftifine HCl) can be fungicidal as well as fungistatic to yeasts depending on the concentration and the organisms involved.

Vismodegib (GDC-0449) is a hedgehog pathway inhibitor (IC50: 3 nM). It also inhibits P-gp (IC50: 3.0 μM), ABCG2 (IC50: 1.4 μM).

Ciliobrevin D is a AAA+ ATPase motor cytoplasmic dynein inhibitor. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation and it also inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.

Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo. It also is an inducer of osteoblast differentiation.

Sonidegib (Erismodegib), a Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.

SANT-1 directly binds to Smoothened (Smo) receptor (Kd: 1.2 nM) and inhibits Smo agonist effects (IC50: 20 nM).

Cyclopamine (11-Deoxojervine), a Smoothened (Smo) antagonist (IC50: 46 nM in TM3Hh12 cells), belongs to the group of steroidal jerveratrum alkaloids.

GANT 61 (GANT61) is an inhibitor for Gli1 and Gli2.

HhAntag is a small molecule inhibitor of GLI1-mediated transcription, an essential down-stream element of the Hedgehog (Hh) pathway with the anti-tumor activity.

MRT-10 is a Smoothened (Smo) receptor antagonist.

SMO-IN-2 is a potent smoothened (SMO) inhibitor of hedgehog (Hh) signaling.SMO-IN-2 shows antiproliferative activity and anticancer activity against human medulloblastoma cell lines.SMO-IN-2 can be used in the study of cancer.

MRT-14 is a potent Smo antagonist and can be used in several types of cancers linked to abnormal Hh signaling studies.

RU-SKI 43 hydrochloride is a potent and selective inhibitor of Hedgehog acyltransferase (Hhat) with an IC50 of 850 nM and exhibits anti-cancer activity.

ALLO-2 is a Inhibitor of Drug-Resistant Smo Mutant.It inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.

Dynarrestin is an inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells. It inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-depen