Smo Inhibitor

Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC₅₀ of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.

Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC₅₀ of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma.

Taladegib (LY2940680) hydrochloride is a Smoothened (SMO) antagonist. Taladegib hydrochloride inhibits the Hedgehog signaling pathway, with an IC₅₀ of 5.5 nM for suppressing GLI1 mRNA expression in DAOY cells and an IC₅₀ of 7.6 nM in CGNP cell proliferation assays. Taladegib hydrochloride binds to the extracellular loop region (site 1) of the transmembrane domain of the SMO receptor, competes with cyclopamine for SMO binding, and thereby inhibits Gli-dependent transcription. Taladegib hydrochloride can be used in studies of Hedgehog pathway-related cancers.

DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ. DY131 also inhibits Smo signaling.

Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC₅₀ of 4 nM.

Taladegib is a Smoothened (SMO) antagonist. Taladegib hydrochloride inhibits the Hedgehog signaling pathway, with an IC₅₀ of 5.5 nM for suppressing GLI1 mRNA expression in DAOY cells and an IC₅₀ of 7.6 nM in CGNP cell proliferation assays. Taladegib binds to the extracellular loop region (site 1) of the transmembrane domain of the SMO receptor, competes with cyclopamine for SMO binding, and thereby inhibits Gli-dependent transcription. Taladegib can be used in studies of Hedgehog pathway-related cancers.

BMS-833923 (XL-139) is an orally biocompatible Smoothened (Smo) inhibitor with anti-tumor activity. It can inhibit the binding of BODIPY cyclopamine to SMO in a dose-dependent manner with an IC₅₀ of 21 nM.

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 nigrum. Jervine has anti-inflammatory and antioxidant properties.

Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.

Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT_2C receptor with an EC₅₀ of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB).

JNJ-1289 is a potent, selective, competitive and allosteric human spermine oxidase (hSMOX) inhibitor (IC₅₀: 50 nM). JNJ-1289 can be used in the research of polyamine catabolism, inflammation and cancers.

LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC₅₀s of 2 and 4 nM in human and mouse, respectively.

CUR61414 is a novel, potent and cell permeable Hedgehog signaling pathway inhibitor (IC₅₀ =100-200 nM). CUR61414 is a small-molecule aminoproline class compound and selectively binds to smoothened (Smo) with a K_i value of 44 nM. CUR-61414 can induce apoptosis in cancer cells without affecting neighboring non-tumor cells.

SMANT hydrochloride is a Smoothened (Smo) signaling inhibitor. SMANT hydrochloride is antagonist of Smo accumulation within the primary cilium (PC). SMANT hydrochloride has an equivalent activity in inhibiting SmoM2 (oncogenic form of Smo) and wild-type Smo.

Glasdegib maleate (PF-04449913 maleate) is a potent and orally bioavailable smoothened inhibitor. Glasdegib maleate binds to human SMO (amino acids 181-787) with IC₅₀value of 4 nM.

SMO-IN-3 (compound 12a) is a potent smoothened (SMO) inhibitor with an IC₅₀ value of 34.09 nM for hedgehog (Hh) signaling pathway. SMO-IN-3 has antiproliferative activity against human medulloblastoma cell line Daoy. Anticancer activity.

Jervine (Standard) is the analytical standard of Jervine. This product is intended for research and analytical applications. 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 nigrum. Jervine has anti-inflammatory and antioxidant properties.

SMO-IN-5 ((Compound 25(B31)) is a potent and competitive inhibitor of smoothened (SMO) that can inhibit Hedgehog (Hh) signaling. SMO-IN-5 interacts with Smo through hydrogen bonds, hydrophobic interactions, and electrostatic forces. SMO-IN-5 inhibits PC cell proliferation, migration, and induces apoptosis by suppressing Gli1 expression. SMO-IN-5 exhibits antitumor activity in pancreatic cancer..

Cyclopamine (Standard) is the analytical standard of Cyclopamine. This product is intended for research and analytical applications. Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.

Glasdegib hydrochloride is a potent and orally bioavailable smoothened inhibitor. Glasdegib hydrochloride (PF-04449913) binds to human SMO (amino acids 181-787) with an IC₅₀ of 4 nM.