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Glasdegib (PF-04449913) inhibits sonic hedgehog (Shh) stimulated luciferase expression in mouse embryonic fibroblasts with an IC50 of 6.8 nM. In vitro microsomal assays, PF-04449913 have high clearance in rat and low clearance in dog and human, without inhibiting any of the major cytochrome P450 isoforms.
In vivo, CD34+ cord blood engrafted NSG mice are treated with Glasdegib (PF-04449913), the frequency of human CD45+ cells, progenitors and both myeloid and lymphoid cell fate commitment remained comparable to vehicle treated controls indicating that unlike LSC, normal human HSC cell fate decisions are Hh pathway independent.
| Molecular Weight | 374.44 |
| Formula | C21H22N6O |
| CAS Number | 1095173-27-5 |
| Solubility (25°C) | DMSO: ≥ 65 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Sadarangani A, et al. J Transl Med. GLI2 inhibition abrogates human leukemia stem cell dormancy.
| Related Smo Products |
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| 20α-Hydroxycholesterol
20α-Hydroxycholesterol is an allosteric activator that selectively targets the Smoothened (Smo) of the Hedgehog pathway with an EC50 of ~30 μM (Hedgehog). 20α-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo in a stereoselective manner, activating downstream Gli transcription factors. 20α-Hydroxycholesterol enhances osteogenic differentiation of bone marrow stromal cells. |
| Glasdegib Maleate
Glasdegib Maleate is an orally bioavailable Smoothened (Smo) inhibitor with an IC50 value of 4 nM for studies related to acute myeloid leukemia. |
| MRT-81
MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer. |
| Fluticasone
Fluticasone is a corticosteroid and Smo agonist with an IC50 of 99 nM, which activates the Hedgehog signaling pathway and promotes the proliferation of primary neural stem or precursor cells, and can be used in respiratory related studies. |
| HhAntag
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway. |
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