PHENOL,2,2'-SULFONYLBIS[3,4,6-TRICHLORO]-

PHENOL,2,2'-SULFONYLBIS[3,4,6-TRICHLORO]- 화학적 특성, 용도, 생산

• 용도

  p38 MAP Kinase Inhibitor IV is an ATP-competitive p38α/β MAPK inhibitor.

• 일반 설명

  A cell-permeable symmetrical sulfone compound that acts as a potent and ATP-competitive inhibitor of p38α/β MAPK (IC₅₀ = 130 and 550 nM, respectively), while exihibiting much reduced activity (≤23% inhibition at 1 μM) against p38γ/δ, ERK1/2, and JNK1/2/3. Shown to be more effective than SB 203850 (Cat. Nos. 559389, 559395, and 559398) in inhibiting LPS-induced IL-1β release from hPBMC (100% vs. 50% inhibition with 100 μM respective inhibitor).

• Biochem/physiol Actions

  p38 MAP Kinase Inhibitor IV is an ATP-competitive inhibitor of p38α/β MAPK with IC50 values of 130 nM for p38α and 550 nM for p38β. It is much less active with ≤23% inhibition at 1 μM against p38γ/σ, ERK1/2, and JNK1/2/3. Shown to be more effective than SB 203580 in inhibiting LPS-induced IL-1β release from hPBMC (100% vs. 50% inhibition with 100 μM inhibitor). A recent study showed that p38 MAP Kinase Inhibitor IV could consistently and significantly enhance reprogramming and iPS cell generation from somatic cells.

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