SB242235
- Product Name
- SB242235
- CAS No.
- 193746-75-7
- Chemical Name
- SB242235
- Synonyms
- CS-668;SB242235;SB242235 ≥95%;SB-242235; SB242235;SB 242235, 10 mM in DMSO;inhibit,SB 242235,Autophagy,Inhibitor,p38 MAPK;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;Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy-
- CBNumber
- CB12621150
- Molecular Formula
- C19H20FN5O
- Formula Weight
- 353.39
- MOL File
- 193746-75-7.mol
SB242235 Property
- 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
Safety
- HS Code
- 2924297099
N-Bromosuccinimide Price
- Product number
- 474182
- Product name
- SB 242235
- Packaging
- 100mg
- Price
- $1848
- Updated
- 2021/12/16
- Product number
- orb180841
- Product name
- SB242235
- Purity
- >98%
- Packaging
- 1000mg
- Price
- $2395.3
- Updated
- 2021/12/16
- Product number
- 132624
- Product name
- 4-(4-(4-Fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl)-2-methoxypyrimidine
- Purity
- 97%
- Packaging
- 5g
- Price
- $3960
- Updated
- 2021/12/16
- Product number
- 3254AH
- Product name
- 4-(4-(4-Fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl)-2-methoxypyrimidine
- Packaging
- 5g
- Price
- $5396
- Updated
- 2021/12/16
- Product number
- 132624
- Product name
- 4-(4-(4-Fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl)-2-methoxypyrimidine
- Purity
- 97%
- Packaging
- 10g
- Price
- $6480
- Updated
- 2021/12/16
SB242235 Chemical Properties,Usage,Production
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
| Cell Line: | Human chondrocytes |
| Concentration: | 0 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM |
| Incubation Time: | < td class="col2"> 15 minutes|
| 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
SB242235 Preparation Products And Raw materials
Raw materials
Preparation Products
SB242235 Suppliers
- Tel
- --
- Fax
- --
- info@chemsworth.com
- Country
- India
- ProdList
- 6700
- Advantage
- 30