Bioactivity | SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC50 of 110 nM for p38α[1][2]. | ||||||||||||
Target | IC50: 110 nM (p38 MAPK). | ||||||||||||
Invitro | SD 0006 clearly inhibits p38α as shown by the dose-dependent inhibition of phosphorylation of its endogenous Hsp27 substrate[1]. | ||||||||||||
In Vivo | SD 0006 (0-30 mg/kg) may be an effective alternative to steroids and biologics for RA therapy[1].SD0006 (3.75, 7.5 and 15 mg/kg; p.o.; b.i.d.) is highly effective in attenuating SCW-induced inflammation as shown by the dose-dependent inhibition of paw swelling[1]. Animal Model: | ||||||||||||
Name | SD 0006 | ||||||||||||
CAS | 271576-80-8 | ||||||||||||
Formula | C20H20ClN5O2 | ||||||||||||
Molar Mass | 397.86 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Burnette BL, et al. SD0006: a potent, selective and orally available inhibitor of p38 kinase. Pharmacology. 2009;84(1):42-60. [2]. Walker JK, et al. Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2634-8. |