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PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ± 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ± 1.4 nmol/L in cells. The μ-opioid receptor is weakly inhibited by PF-5274857 with a dissociation constant of 36 μM subsequently determined in a functional assay. PF-5274857 was orally available and metabolically stable in vivo. PF-5274857 shows significant dose-dependent tumor growth inhibition (TGI) and induces tumor regression at high doses(>10 mg/kg). PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hedgehog (Hh) signaling pathway. PF-5274857 is also able to cross the blood–brain barrier in rats within 4 hours post-dose.
| Molecular Weight | 436.96 |
| Formula | C20H25ClN4O3S |
| CAS Number | 1373615-35-0 |
| Solubility (25°C) | DMSO 80 mg/mL Water 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Hedgehog Products |
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| TPB15
TPB15 is an orally potent Hh (Hedgehog) signaling inhibitor that significantly induces MDA-MB-468 cell cycle arrest and apoptosis. TPB15 also blocks Smo (Smoothened) translocation into cilia and reduces Smo protein and mRNA expression. In addition, TPB15 can inhibit the expression of downstream regulator Glioma-associated oncogene 1 (Gli1). TPB15 has good anti-tumor activity and low toxicity. |
| Hedgehog IN-3
Hedgehog IN-3 is a hedgehog pathway inhibitor (IC50 = 0.01 µM). |
| Hedgehog IN-5
Hedgehog IN-5 is an orally active small molecule inhibitor of the hedgehog pathway. |
| Hedgehog IN-2
Hedgehog IN-2 is an inhibitor of Hedgehog pathway with an IC50 value less than 0.003 μM in C3H10T1/2 cells. |
| Physalin H
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. |
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