1204975-42-7
1204975-42-7 structure
- Name: LEQ506
- Chemical Name: 2-[(R)-4-(6-benzyl-4,5-dimethyl-pyridazin-3-yl)-2-methyl-3,4,5,6-tetrahydro-2H-[1,2']bipyrazinyl-5'-yl]-propan-2-ol
- CAS Number: 1204975-42-7
- Molecular Formula: C25H32N6O
- Molecular Weight: 432.56100
- Catalog: Signaling Pathways Stem Cell/Wnt Smo
- Create Date: 2018-02-19 23:25:52
- Modify Date: 2024-01-10 18:39:44
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LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.
| Name | 2-[(R)-4-(6-benzyl-4,5-dimethyl-pyridazin-3-yl)-2-methyl-3,4,5,6-tetrahydro-2H-[1,2']bipyrazinyl-5'-yl]-propan-2-ol |
|---|---|
| Synonyms |
(R)-2-(5-(4-(6-benzyl-4,5-dimethylpyridazin-3-yl)-2-methylpiperazin-1-yl)pyrazin-2-yl)propan-2-ol
LEQ506 |
| Description | LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively. |
|---|---|
| Related Catalog | |
| Target |
IC50: 2 nM (human smo), 4 nM (mouse smo)[1] |
| In Vitro | LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively. LEQ506 inhibits Hedgehog (Hh) signaling in a human cell line (HEPM) as measured by the amount of Gli mRNA with an IC50 ~6-fold lower than that of Compound 2[1]. LEQ506 is an efficacious compound by consistently decreasing Gli1 mRNA by about 70 to 80%. LEQ506 shows a tendency to preferentially inhibit Gli1 rather than Ptch1 mRNA. LEQ506 (at 1%) is also an efficacious compound with an inhibition of 80 to 90% for Gli1 and of 60 to 70% for Ptch1[2]. |
| Cell Assay | DAOY cells are serum starved 16 h before experiments and subsequently incubated for 24 h with sonic Hedgehog (SHH) (50 nM) and LEQ506 at different concentrations. Cells are then washed twice with PBS and stored at -80°C until RNA isolation. Total RNA is isolated using the RNeasy Mini Kit. The amount and quality of extracted RNA are determined using the 2100 Bioanalyzer[2]. |
| References |
| Molecular Formula | C25H32N6O |
|---|---|
| Molecular Weight | 432.56100 |
| Exact Mass | 432.26400 |
| PSA | 78.27000 |
| LogP | 3.54670 |
| Storage condition | 2-8℃ |