211555-05-4
211555-05-4 structure
- Name: WHI-P97
- Chemical Name: 2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
- CAS Number: 211555-05-4
- Molecular Formula: C16H13Br2N3O3
- Molecular Weight: 455.10100
- Catalog: Biochemical Inhibitor Protein tyrosine kinase
- Create Date: 2019-01-01 20:33:19
- Modify Date: 2025-08-27 12:18:57
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WHI-P97 is a rationally designed potent inhibitor of JAK-3.IC50 value:Target: JAK3Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal. WHI-P97 was very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 microg/kg to 50 mg/kg, and LD(10) was not reached at a 50 mg/kg dose level when administered as a single i. p. or i.v. bolus dose.
| Name | 2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol |
|---|---|
| Synonyms |
whi-p97
hms3265e23 |
| Description | WHI-P97 is a rationally designed potent inhibitor of JAK-3.IC50 value:Target: JAK3Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal. WHI-P97 was very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 microg/kg to 50 mg/kg, and LD(10) was not reached at a 50 mg/kg dose level when administered as a single i. p. or i.v. bolus dose. |
|---|---|
| Related Catalog | |
| Target |
JAK3:11 μM (IC50) |
| References |
| Density | 1.785 |
|---|---|
| Molecular Formula | C16H13Br2N3O3 |
| Molecular Weight | 455.10100 |
| Exact Mass | 452.93200 |
| PSA | 76.50000 |
| LogP | 4.69420 |
| Storage condition | -20°C |