Hedgehog Inhibitor

Hedgehog IN-6 (Compound Q29) is a Hedgehog (Hh) inhibitor that can be used in cancer research. Hedgehog IN-6 inhibits the hedgehog (Hh) pathway by binding to the cysteine-rich domain (CRD) of Smoothened (Smo) and blocking its cholesterization.

NL-103 is an inhibitor of histone deacetylases (HDACs) and Hedgehog, with the IC₅₀ values ​​of 21.3 nM, 57 nM, 74 nM, and 680 nM for HDAC1, HDAC2, HDAC3, and HDAC6, respectively. NL-103 can downregulate the expression of Gli2. NL-103 can be used in anti-cancer research.

Garcinone C (Standard) is the analytical standard of Garcinone C. This product is intended for research and analytical applications. Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active.

HPP-9 is a Proteolysis-Targeting Chimeras （PROTACs） based on Hedgehog Pathway Inhibitor-1 (HPI-1), with the pIC₅₀ of 6.71, that can degrade BET bromodomains. HPP-9 has antitumor activity^[1[.

Hedgehog IN-3 (compound 3) is a hedgehog pathway inhibitor (IC₅₀ = 0.01 µM). Hedgehog IN-3 can be used in cancer research.

Hedgehog IN-10 (compound 24) is a potent Hedgehog inhibitor. Hedgehog IN-10 exhibits significant antitumor effect.

Hedgehog IN-11 is an orally active Hedgehog inhibitor. Hedgehog IN-11 downregulates the expression of O6-methylguanine-DNA methyltransferase (MGMT) to impair the Temozolomide (TMZ) (HY-17364) resistance by inhibiting the Hedgehog pathway. Hedgehog IN-11 shows improved inhibition of cell migration and invasion, and induced cell apoptosis in TMZ-resistant GBM cell lines. Hedgehog IN-11 is predicted by computer simulation to have good blood-brain barrier penetration. Hedgehog IN-11 can be used for the study of glioblastoma (GBM).

Physalin H is a natural product that can be isolated from Solanum nigrum. Physalin H is an inhibitor of Hedgehog (Hh) signaling and it disrupts GLI1-DNA-complex formation. Physalin H inhibits GLI1 transcription with an IC₅₀ value of 0.7 μM. Physalin H shows cytotoxicity to PANC1 and DU145 cells with IC₅₀ values of 5.7 and 6.8 μM, respectively.

Hedgehog IN-9 (Compound 1) is a Hedgehog inhibitor. Hedgehog IN-9 prevents GLI1 expression and enhances cellular BRD2 protein levels. Hedgehog IN-9 inhibits growth of medulloblastoma spheroid cells and can be used for synthesis of photoaffinity labeling probe.

MEDI-5304 is a hedgehog antibody inhibitor with human sonic hedgehog (SHH) K_D of 5.13 pmol/L, and human Indian hedgehog (IHH) K_D of 34.7 pmol/L. MEDI-5304 binds and neutralizes SHH and IHH, blocks downstream target gene transcription, inhibits osteoblast differentiation. MEDI-5304 can be used for the research of colon cancer.

HSP70-IN-3 is a potent HSP70 inhibitor (IC₅₀s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1.

TPB15 is an orally active and potent Hh (Hedgehog) signaling inhibitor. TPB15 markedly induces cell cycle arrest and apoptosis in MDA-MB-468 cells. TPB15 blocks Smo (Smoothened) translocation into the cilia and reduced Smo protein and mRNA expression. TPB15 inhibits the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1). TPB15 shows good anti-tumor activity with low toxicity.

Hedgehog IN-7 (Compound 8g), a purine derivative, acts as an inhibitor of Hedgehog, capable of reducing the expression of Hedgehog genes and inhibiting Hedgehog signaling. Hedgehog IN-7 has significant cytotoxicity and selectivity towards the Hedgehog pathway-dependent pancreatic cancer cell Mia-PaCa-2 cells and can be used in the research of pancreatic cancer.

Ornidazole-¹³C₂,¹⁵N₂ is the ¹³C, ¹⁵N labeled Ornidazole. Ornidazole (Ro 7-0207) is a nitroimidazole derivative with anti-trichomonad activity and in vitro activity against a variety of anaerobic bacteria. Ornidazole inhibits Sonic hedgehog (Shh) signaling pathway, exhibits antitumor activity. Ornidazole can be used in research of Crohn’s disease.

CBR-096-4 is a derivative of Itraconazole (HY-17514). CBR-096-4 is an orally active antifibrotic agent with no CYP3A4 inhibitory activity. CBR-096-4 inhibits the formation of matrix-secreting activated myofibroblasts (MFBs) from multiple tissue types. CBR-096-4 inhibits Hedgehog reporter activity (GLI-LUC), VEGF-dependent growth, and αSMA-LUC reporter activity. CBR-096-4 can be used for research of fibrosis.

Hedgehog IN-5 is an orally active small molecule inhibitor of the hedgehog pathway. Hedgehog IN-5 can be used for the research of fibrotic disease.

Hedgehog IN-4 is a benzamide derivative and also an inhibitor of the Hedgehog signaling pathway, with an IC₅₀ of 0.050 nM.

Vismodegib (Standard) is the analytical standard of Vismodegib. This product is intended for research and analytical applications. Vismodegib (GDC-0449) is a BBB-permeable and orally active hedgehog pathway inhibitor with an IC₅₀ of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC₅₀ values of 3.0 μM and 1.4 μM, respectively.

Jervine hydriodide (11-Ketocyclopamine hydriodide) is an orally active steroidal alkaloid and Hedgehog signaling pathway inhibitor. Jervine hydriodide can be isolated from Veratrum californicum. Jervine hydriodide regulates Wnt, inhibits the AKT/mTOR signaling pathway, and activates the AMPK signaling pathway. Jervine hydriodide induces DNA damage, Apoptosis, Autophagy, ROS production and Mitochondrial damage. Jervine hydriodide exhibits anti-cancer and anti-inflammatory activities. Jervine hydriodide reduces tumor growth rate and weight in xenograft models. Jervine hydriodide can be used in studies related to triple-negative breast cancer, nasopharyngeal carcinoma and non-small cell lung cancer.

Ornidazole (Standard) is the analytical standard of Ornidazole. This product is intended for research and analytical applications. Ornidazole (Ro 7-0207) is a nitroimidazole derivative with anti-trichomonad activity and in vitro activity against a variety of anaerobic bacteria. Ornidazole inhibits Sonic hedgehog (Shh) signaling pathway, exhibits antitumor activity. Ornidazole can be used in research of Crohn’s disease.