1983136-72-6
1983136-72-6 structure
- Name: (R)-STU104
- Chemical Name: (R)-STU104
- CAS Number: 1983136-72-6
- Molecular Formula: C18H18O4
- Molecular Weight: 298.338
- Create Date: 2022-07-10 12:01:31
- Modify Date: 2024-04-02 13:12:37
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(R)-STU104 is a potent, first-in-class TAK1-MKK3 porotein-protein interaction (PPI) inhibitor with SPR Kd of 71 nM for binding MKK3, disrupting the TAK1 phosphorylating MKK3.(R)-STU104 exhibited the potent inhibitory activity on TNF-α production on RAW264.7 cells with IC50 of 0.58 uM, suppressed the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways.(R)-STU104 demonstrated remarkable dose-effect relationships on both acute and chronic mouse ulcerative colitis (UC) models.(R)-STU104 showed better anti-UC efficacy in vivo at 10 mg/kg/d than mesalazine at the dose of 50 mg/kg/d.
| Name | (R)-STU104 |
|---|
| Description | (R)-STU104 is a potent, first-in-class TAK1-MKK3 porotein-protein interaction (PPI) inhibitor with SPR Kd of 71 nM for binding MKK3, disrupting the TAK1 phosphorylating MKK3.(R)-STU104 exhibited the potent inhibitory activity on TNF-α production on RAW264.7 cells with IC50 of 0.58 uM, suppressed the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways.(R)-STU104 demonstrated remarkable dose-effect relationships on both acute and chronic mouse ulcerative colitis (UC) models.(R)-STU104 showed better anti-UC efficacy in vivo at 10 mg/kg/d than mesalazine at the dose of 50 mg/kg/d. |
|---|---|
| References | 1. Mei-Lin Tang, et al. J Med Chem. 2022 Apr 20. doi: 10.1021/acs.jmedchem.1c02198. |
| Molecular Formula | C18H18O4 |
|---|---|
| Molecular Weight | 298.338 |