Basic information Safety Supplier Related

SB242235

Basic information Safety Supplier Related

SB242235 Basic information

Product Name:
SB242235
Synonyms:
  • SB-242235; SB242235
  • CS-668
  • SB242235
  • 4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxypyrimidine
  • 4-(4-(4-Fluorophenyl)-1-(piperidin-4-yl)-1H-iMidazol-5-yl)-2-MethoxypyriMidine
  • SB242235 ≥95%
  • Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy-
  • inhibit,SB 242235,Autophagy,Inhibitor,p38 MAPK
CAS:
193746-75-7
MF:
C19H20FN5O
MW:
353.39
Mol File:
193746-75-7.mol
More
Less

SB242235 Chemical Properties

Boiling point:
568.4±60.0 °C(Predicted)
Density 
1.34
storage temp. 
2-8°C(protect from light)
solubility 
DMF: 25 mg/ml; DMSO: 20 mg/ml; Ethanol: 30 mg/ml
form 
Powder
pka
9.91±0.10(Predicted)
color 
White to off-white
More
Less

Safety Information

HS Code 
2924297099
More
Less

SB242235 Usage And Synthesis

Uses

SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0　μM in primary human chondrocytes[1].

Biological Activity

SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 μM in human chondrocytes.

in vitro

SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC 50 of 1.0 μM in human chondrocytes stimulated with IL-1β.
SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate.

Western Blot Analysis

< td class="col2"> 15 minutes
Cell Line: Human chondrocytes
Concentration: 0 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time:
Result: Dose-dependently inhibited the activation of MAPKAP K2 with an IC 50 of 1.0 μM.

in vivo

SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation[2].
SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2[2].
SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey[3].

Animal Model:Female SKH-1 hairless mice (4–6 weeks)[2]
Dosage:100 mg/kg
Administration:Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation
Result:Abolished MAP-KAPK-2 activity and heat shock protein 27 (HSP27) phosphorylation.

target

IC50: 1.0 μM (p38 MAPK, primary human chondrocytes)

References

[1] Badger, A.M., et al., Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte cultures. Osteoarthritis Cartilage, 2000. 8(6): p. 434-43. DOI:10.1053/joca.1999.0319
[2] Kim AL , et al. Role of p38 MAPK in UVB-induced inflammatory responses in the skin of SKH-1 hairless mice. J Invest Dermatol. 2005 Jun;124(6):1318-25. DOI:10.1111/j.0022-202X.2005.23747.x
[3] Ward, K.W., et al., SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. I: preclinical pharmacokinetics. Xenobiotica, 2002. 32(3): p. 221-33. DOI:10.1080/00498250110100720

SB242235Supplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Email
info@chemexpress.com
SYN|thesis med chem P/L
Tel
+86-021-50720296
Email
service@synkinase.com
ShangHai YingYi Chemical Technology Co., Ltd.
Tel
86-21-50700185 13764109623
Email
sale@inyelchem.com
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Email
info@adooq.cn
More
Less

SB242235(193746-75-7)Related Product Information