Product Name :
PD 198306
Description:
IC50: 8 nM for MEK PD 198306 is a potent, selective and non-ATP competitive MAPK/ERK-kinase (MEK) inhibitor. MEK is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). In vitro: PD 198306 inhibits the isolated MEK at a concentration of 8 nM and inhibits MEK activity in synovial fibroblasts at 30–100 nM, depending on the species. PD 198306 is highly selective for MEK and has a IC50 of >4 uM for c-Src, >1 uM for ERK, >4 uM for cyclin-dependent kinases and >10 uM for phosphatidylinositol 3-kinase . In vivo: Rabbits treated with PD 198306 showd a significant dose-dependent reduction in the level of phospho-ERK-1/2 and a lower level of MMP-1. PD 198306 can partially decrease the development of some of the structural changes in experimental rabbit model of osteoarthritis . PD 198306 dose-dependently blocked static allodynia in both the streptozocin and the chronic constriction injury models of neuropathic pain. These antihyperalgesic effects correlated with a reduction in the elevated levels of active ERK1 and 2 in lumbar spinal cord . Clinical trial: So far, no clinical study has been conducted.
CAS:
212631-61-3
Molecular Weight:
476.23
Formula:
C18H16F3IN2O2
Chemical Name:
N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]benzamide
Smiles :
CC1=CC(I)=CC=C1NC1=C(C=C(F)C(F)=C1F)C(=O)NOCC1CC1
InChiKey:
UHAXDAKQGVISBZ-UHFFFAOYSA-N
InChi :
InChI=1S/C18H16F3IN2O2/c1-9-6-11(22)4-5-14(9)23-17-12(7-13(19)15(20)16(17)21)18(25)24-26-8-10-2-3-10/h4-7,10,23H,2-3,8H2,1H3,(H,24,25)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{HPPE} site|{HPPE} Metabolic Enzyme/Protease|{HPPE} TGF-beta/Smad|{HPPE} Protocol|{HPPE} In stock|{HPPE} custom synthesis}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
IC50: 8 nM for MEK PD 198306 is a potent, selective and non-ATP competitive MAPK/ERK-kinase (MEK) inhibitor.{{Dolutegravir} medchemexpress|{Dolutegravir} HIV Integrase|{Dolutegravir} Purity & Documentation|{Dolutegravir} Description|{Dolutegravir} custom synthesis|{Dolutegravir} Autophagy} MEK is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). In vitro: PD 198306 inhibits the isolated MEK at a concentration of 8 nM and inhibits MEK activity in synovial fibroblasts at 30–100 nM, depending on the species. PD 198306 is highly selective for MEK and has a IC50 of >4 uM for c-Src, >1 uM for ERK, >4 uM for cyclin-dependent kinases and >10 uM for phosphatidylinositol 3-kinase . In vivo: Rabbits treated with PD 198306 showd a significant dose-dependent reduction in the level of phospho-ERK-1/2 and a lower level of MMP-1.PMID:32180353 PD 198306 can partially decrease the development of some of the structural changes in experimental rabbit model of osteoarthritis . PD 198306 dose-dependently blocked static allodynia in both the streptozocin and the chronic constriction injury models of neuropathic pain. These antihyperalgesic effects correlated with a reduction in the elevated levels of active ERK1 and 2 in lumbar spinal cord . Clinical trial: So far, no clinical study has been conducted.|Product information|CAS Number: 212631-61-3|Molecular Weight: 476.23|Formula: C18H16F3IN2O2|Chemical Name: N-(cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]benzamide|Smiles: CC1=CC(I)=CC=C1NC1=C(C=C(F)C(F)=C1F)C(=O)NOCC1CC1|InChiKey: UHAXDAKQGVISBZ-UHFFFAOYSA-N|InChi: InChI=1S/C18H16F3IN2O2/c1-9-6-11(22)4-5-14(9)23-17-12(7-13(19)15(20)16(17)21)18(25)24-26-8-10-2-3-10/h4-7,10,23H,2-3,8H2,1H3,(H,24,25)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|