hedgehog signaling pathway

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.

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

SAG (Smoothened Agonist) is a Smo receptor agonist (EC50=3 nM) that is cell-permeable and selective. SAG regulates Smo activity by binding directly to the Smo helix and can activate the Hedgehog signaling pathway.

GI-560192 (RL-0070933) is a potent smo cilial modulator with an EC50 value of 0.02 µM. GI-560192 modulates the translocation and or accumulation of smoothened to the primary cilia by hedgehog signaling pathway.

Saridegib is an effective and specific inhibitor of Smoothened and a key signaling transmembrane protein in the Hedgehog pathway.

HedgehogIN-7 (Compound 8g), a purine derivative, acts as an inhibitor of the Hedgehog signaling pathway by reducing the expression of Hedgehog genes and inhibiting signal transmission. This compound exhibits significant cytotoxicity and selectivity towards Mia-PaCa-2 pancreatic cancer cells that are dependent on the Hedgehog pathway, making it useful for research in pancreatic cancer.

MRT-92 is an antagonist of Smoothened (Smo) with anti-cancer activity, featuring a binding affinity (Ki) of 0.7 nM. It inhibits the Hedgehog signaling pathway by obstructing the overlapping binding sites within the transmembrane domain of the Smoothened receptor and suppresses the proliferation of cerebellar granule cells in rodents (IC50=0.4 nM). MRT-92 is utilized for research into cerebellar gliomas.

1-Methyladenosine-d3 hydrochloride is the hydrochloride salt form of deuterium-labeled 1-Methyladenosine. This compound is a modification of RNA that serves as a biomarker for tumors, with elevated levels in the body linked to cancer development. Upon methylation, 1-Methyladenosine upregulates the expression of PPARδ, regulates cholesterol metabolism, and activates the Hedgehog signaling pathway, thereby driving the onset of liver tumors.

7-Keto-27-hydroxycholesterol is a significant bioactive compound known for its ability to activate the smoothened (SMO) protein within the Hedgehog (Hh) signaling pathway, which is crucial for proper cell differentiation in embryonic tissues.

SMO-IN-5 (Compound 25(B31)) is an effective inhibitor of smoothened (SMO), which suppresses the Hedgehog (Hh) signaling pathway. This compound inhibits cellular proliferation and induces apoptosis, demonstrating antitumor activity.

1-Methyladenosine-d3 hydriodide is the deuterated form of 1-Methyladenosine. This compound is an RNA modification and serves as a tumor marker, with elevated levels in the body linked to cancer development. Methylated 1-Methyladenosine can promote liver tumor development by upregulating PPARδ expression, regulating cholesterol metabolism, and activating the Hedgehog signaling pathway.

Eggmanone (EGM1) is a potent, selective phosphodiesterase 4 (PDE4) antagonist, exhibiting an IC50 of 72 nM specifically for PDE4D3. It shows 40- to 50-fold greater selectivity for PDE4D3 over other phosphodiesterases. The mechanism of action involves PDE4 selective antagonism by Eggmanone, which activates protein kinase A, culminating in the blockade of the Hedgehog (Hh) signaling pathway [1].

HPI 1 is a hedgehog (Hh) signaling inhibitor. Inhibits Sonic hedgehog (Shh)-, SAG- and Gli-induced Hh pathway activation in Shh-LIGHT2 cells (IC50 values are 1.5, 1.5, 4, and 6 μM for Shh-, SAG-, Gli2- and Gli1-induced activation).

SANT 2 is a Hedgehog (Hh) signaling pathway antagonist with potential anti-inflammatory and anticancer activity for the study of prostate, pancreatic and breast cancer.

PF-5274857 is a potent, orally active and selective inhibitor of hedgehog (Hh) signaling pathway (IC50 = 5.8 nM, Ki = 4.6 nM) . PF-5274857 effectively penetrates the blood-brain barrier and inhibits Smo activity in the brain of primary medulloblastoma mic

Ciliobrevin A (HPI-4) is an inhibitor of the hedgehog signaling pathway with an IC50 of less than 10 μM.

Jervine is a naturally occurring steroidal alkaloid derived from the Veratrum plant species. Over the Hedgehog signaling pathway, Jervine effectively inhibits tumor growth using three human tumor xenograft models. Jervine has the potential to advance to t

HPI-1 (hydrate) is a Hedgehog (Hh) pathway inhibitor that suppresses signaling through Sonic Hh (IC50= 1.5 μM) without significantly affecting Wnt signaling (IC50≥ 30 μM).1HPI-1 suppresses Hh activation induced by loss of Suppressor of Fused or by Gli overexpression, suggesting action at posttranslational modification of Gli protein or at the interaction of Gli with a co-factor.1HPI-1 (hydrate) also inhibits signaling through the oncogenic Smoothened (Smo) mutant SmoM2 in neuron precursors, preventing cell proliferation.1 1.Hyman, J.M., Firestone, A.J., Heine, V.M., et al.Small-molecule inhibitors reveal multiple strategies for Hedgehog pathway blockadeProceedings of the National Academy of Sciences of the United States of America106(33)14132-14137(2009)

Potent fluorescent Smo antagonist (IC50 = 100 nM). Non-fluorescent analog also available. Fan et al (2014) The Hedgehog pathway effector smoothened exhibits signaling competency in the absence of ciliary accumulation. Chem.Biol. 21 1680 PMID:25484239

MRT-83 (hydrochloride) is a potent antagonist of the Smoothened (Smo) receptor, effectively inhibiting the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. With its potential applications in the study of cancer disease, MRT-83 (hydrochloride) demonstrates promising prospects for research purposes.

Saponin activator. Activates release of Prostaglandin E2 in vitro. Anti-inflammatory agent. Orally active. Active in vivo and in vitro.

SAG dihydrochloride, a powerful agonist of the Smoothened (Smo) receptor (EC 50 = 3 nM; Kd = 59 nM), effectively activates the Hedgehog signaling pathway. It also negates the effects of Cyclopamine inhibition on Smo.