PD98059
PD98059
CAS: 167869-21-8
Molecular Formula: C16H13NO3
PD98059 - Names and Identifiers
| Name | PD98059 |
| Synonyms | PD98059 PD 98059 PD 098,059 PD 98059 in Solution 2'-AMINO-3'-METHOXYFLAVONE 2-(2-AMINO-3-METHOXY-PHENYL)CHROMEN-4-ONE 2-(2-AMINO-3-METHOXYPHENYL)-4H-CHROMEN-4-ONE 2-(2-AMINO-3-METHOXYPHENYL)-4H-1-BENZOPYRAN-4-ONE PD 098,059 (2-(2-AMINO-3-METHOXYPHENYL)- 4H-1-BENZOPYRAN-4-ONE |
| CAS | 167869-21-8 |
| InChIKey | QFWCYNPOPKQOKV-UHFFFAOYSA-N |
PD98059 - Physico-chemical Properties
| Molecular Formula | C16H13NO3 |
| Molar Mass | 267.28 |
| Density | 1.300±0.06 g/cm3(Predicted) |
| Melting Point | 164～165℃ |
| Boling Point | 453.1±45.0 °C(Predicted) |
| Solubility | Soluble in DMSO (6.5 mg/ml), anhydrous DMSO (25 mg/ml), ethanol (0.6 mg/ml), dichloromet |
| Appearance | Yellow solid |
| Color | yellow |
| pKa | 1.21±0.10(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Sensitive | Sensitive to heat |
| MDL | MFCD00671789 |
| Use | A selective inhibitor of MEK and blocker of MAP |
| In vitro study | PD98059 either inhibits background MEK1 or a partially activated MEK mutant formed by mutating serine to glutamate at positions 218 and 222 (MEK-2E), IC50 is 2 μm. PD98059 does not inhibit the two MAPK homologs of JNK and p38. PD98059 is highly selective for inhibiting MEK, as it is highly selective for others including Raf kinase, cAMP-dependent kinase, protein kinase C, v-Src, epidermal growth factor (EGF) receptor kinase, insulin receptor kinase, PDGF receptor kinase, and phosphatidylinositol (-3) kinase, including a series of kinases are not inhibitory. PD98059 inhibited the entry of MAPK and thymidine activated by PDGF stimulation into 3T3 cells with IC50 of ~ 10 μm and ~ 7 μm, respectively. PD98059 can effectively prevent MEK1 from being activated by Raf or MEK kinase, IC50 is 4 μm, The activation of MEK2 by Raf can be weakly inhibited with an IC50 of 50 μm. In KB and PC12 cells, PD98059 did not inhibit the activation of MKK4 and RK kinases, two homologs of MEK involved in stress-and interleukin-1-mediated kinase cascades, p70 S6 kinase activation was also not inhibited by insulin or epidermal growth factor in Swiss 3T3 cells. PD98059 completely blocked nerve growth factor (NGF)-induced differentiation of PC12 cells without altering cell viability. PD98059 inhibited the proliferation of RAW264.7 cells cultured in medium containing osteoclast differentiation factors in a dose-dependent manner, resulting in a significant decrease in the number of TRAP-positive cells. |
| In vivo study | Treatment of mice with PD98059 30 minutes before Cerebral Ischemia can significantly reduce the injury and reduce the volume of cerebral infarction. Pretreatment with PD98059 (10 mg/kg I. V.) 30 min earlier based on wet weight and histological findings of the pancreas mice that were then injected with bombesin every hour for three consecutive times significantly improved bombesin-induced acute pancreatitis. Treatment of mice with PD98059 (10 mg/kg) one hour after carrageenan injury showed a decrease in all indicators associated with inflammation. |
PD98059 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| Safety Description | S22 - Do not breathe dust. S60 - This material and its container must be disposed of as hazardous waste. S36 - Wear suitable protective clothing. |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| HS Code | 29322090 |
PD98059 - Reference
| Reference Show more | 1. [IF=5.192] Chunliu Mi et al."Digitoxin promotes apoptosis and inhibits proliferation and migration by reducing HIF-1α and STAT3 in KRAS mutant human colon cancer cells."Chem-Biol Interact. 2022 Jan;351:109729 2. [IF=4.36] Jing Han et al."Lingguizhugan decoction protects PC12 cells against Aβ25-35-induced oxidative stress and neuroinflammation by modulating NF-κB/MAPK signaling pathways."J Ethnopharmacol. 2022 Jun;292:115194 |
PD98059 - Introduction
PD 98,059
Last Update：2022-10-16 17:41:28
PD98059 - Reference Information
| biological activity | PD98059 is a non-ATP competitive MEK inhibitor. IC50 is 2 μM in cell-free test, which specifically inhibits MEK-1-mediated MAPK activation. Do not directly inhibit ERK1 or ERK2. PD98059 is a ligand of aryl hydrocarbon receptor (AHR) and acts as an antagonist. |
| Target | Value |
| AhR (Cell-free assay) | 1 μM |
| MEK1 (Cell-free assay) | 2 μM |
Last Update：2024-04-09 21:54:55
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Product Name: PD98059 Visit Supplier Webpage Request for quotationCAS: 167869-21-8
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Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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