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MEK

MEK

MEK (Mitogen-activated protein kinase kinase, MAPKK) is a kinase enzyme which phosphorylates mitogen-activated protein kinases (MAPKs).The downstream transcription factors that control responses like stress signaling, pathogen response, and hormone signaling are phosphorylated as a result of the activated MAPK.

The final protein in the cascade, a MAPK (ERK, p38, or JNK), is activated by the MAPKKK by phosphorylating a serine or threonine residue on a MAPKK. Mitogen-activated protein kinase kinase 3 (MKK3), MKK6, and occasionally MKK4 are primarily responsible for activating the p38 MAPK. Two upstream MAP2Ks, MKK4 and MKK7, control the JNK. Raf and Ras are activated by the highly homologous kinases MEK1 and MEK2, which then activate ERK mitogen-activated protein kinases.

MEK related products

Structure Cat No. Product Name CAS No. Product Description
(R)-PD 0325901CL V74094 (R)-PD 0325901CL 1003216-77-0 (R)-PD 0325901CL is an isomer of PD 0325901CL.
APS-2-79 V3182 APS-2-79 2002381-25-9 APS-2-79 (APS-279) is a potent antagonist of MAPK (mitogen-activated protein kinase) with antitumor activity.
APS-2-79 HCl V2664 APS-2-79 HCl 2002381-31-7 APS-2-79 HCl (APS279 HCl; APS-279), the hydrochloride salt of APS-2-79, is an antagonist of MAPK (mitogen-activated protein kinase) with anticancer effects.
AZD8330 (ARRY704; ARRY424704) V0458 AZD8330 (ARRY704; ARRY424704) 869357-68-6 AZD8330 (AZD-8330; ARRY-704; ARRY-424704) is an orally bioactive and non-ATP competitive (Allosteric) MEK 1/2 inhibitor with potential anticancer activity.
Binimetinib ( Mektovi; ARRY438162; ARRY162; MEK162) V0454 Binimetinib ( Mektovi; ARRY438162; ARRY162; MEK162) 606143-89-9 Binimetinib (trade name:Mektovi; formerly ARRY-438162; ARRY-162; MEK-162) is a highly selective and orally bioavailable MEK1/2(mitogen-activated protein kinase kinase) inhibitor with potential antineoplastic activity.
BIX 02188 V0457 BIX 02188 334949-59-6 BIX02188 (BIX-02188), an indolinone analog, is a novel, highly potent and selective MEK5 inhibitor with the potential to relieve neuropathic pain.
BIX 02189 V0450 BIX 02189 1094614-85-3 BIX02189 is a novel, potent andselective inhibitor of MEK5 with important biological activity.
BIX02189 V33372 BIX02189 1265916-41-3 BIX02189 is a novel, potent and selective MEK5 inhibitor with an IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
Cobimetinib (GDC-0973, RG-7420, XL-518) V0453 Cobimetinib (GDC-0973, RG-7420, XL-518) 934660-93-2 Cobimetinib (formerly GDC0973, RG7420, XL518; trade name Cotellic) is an orally bioavailable and selective small-molecule inhibitor of MEK1 with potential anticancer activity.
Cobimetinib hemifumarate V4524 Cobimetinib hemifumarate 1369665-02-0 Cobimetinib hemifumarate (formerly also known as RG7420; XL518; GDC0973), thehemifumarate salt of cobimetinib, is an oral, highly potent and selective MEK1 inhibitor with potential antineoplastic activity.
Cobimetinib racemate V4523 Cobimetinib racemate 934662-91-6 Cobimetinib racemate is the racemic mixture of Cobimetinib (GDC-0973, RG7420; XL-518; Cotellic), which is a novel, orally bioavailable, highly potent and selective small-molecule MEK1 inhibitor with antitumor activity.
GDC-0623 (G-868) V0451 GDC-0623 (G-868) 1168091-68-6 GDC-0623 (G868) is a novel, potent, orally bioactive, selective and non-ATP-competitive (allosteric) inhibitor of MEK1 with potential anticancer activity.
GSK1790627 V74088 GSK1790627 871701-87-0 GSK1790627 is the N-deacetylated metabolite of trametinib.
GW284543 V4731 GW284543 790186-68-4 GW284543 (also known as GW-284543; UNC10225170; UNC-10225170) is a novel, potent and selectiveMEK5inhibitor with potential usefulness in cancer treatment.
Honokiol (NSC-293100) V0167 Honokiol (NSC-293100) 35354-74-6 Honokiol (also known as NSC 293100) is a naturally-occuring, bioactive, biphenolic phytochemical and an active ingredient of magnolia extract with potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities.
Isorhamnetin V4735 Isorhamnetin 480-19-3 Isorhamnetin (also named as 3-Methylquercetin) is a flavonoid analog isolated from the Chinese herb Hippophae rhamnoides L.
MEK-IN-6 V74092 MEK-IN-6 2845151-86-0 MEK-IN-6 (Example 69) is a MEK inhibitor.
MEK-IN-6 hydrate V74090 MEK-IN-6 hydrate 2845153-35-5 MEK-IN-6 hydrate (compound 69) is a MEK inhibitor.
MEK1/C-Raf-IN-1 V83686 MEK1/C-Raf-IN-1 946128-76-3
MEK4 inhibitor-1 V74091 MEK4 inhibitor-1 2570386-36-4 MEK4 inhibitor-1 is a new MEK4 inhibitor against pancreatic cancer, with IC50 of 61 nM.
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