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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V0445 | Mirdametinib (PD0325901) | 391210-10-9 | Mirdametinib (PD-0325901) is a novel, potent,selective, orally bioavailable and non ATP-competitive inhibitor of the mitogen-activated protein kinaseMEK with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. |
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V74087 | MS934 | 2756323-15-4 | MS934 is a novel improved VHL-recruiting MEK 1/2 degrader. |
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V1991 | Myricetin (Cannabiscetin) | 529-44-2 | Myricetin (Cannabiscetin), a naturally occuring flavonoid with antioxidant and anti tumor properties, is a novel inhibitor of MEK1 activity and transformation of JB6 P+ mouse epidermal cells. |
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V74089 | Nedometinib | 2252314-46-6 | Nedometinib is a tyrosine kinase inhibitor targeting MEK1. |
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V0448 | PD184352 (CI1040) | 212631-79-3 | PD184352 (PD-184352; CI-1040),an analog of benzhydroxamate, is an orally bioactive, specific, allosteric/non-ATP competitive MEK1/2 inhibitor with potential anticancer activity. |
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V0460 | PD318088 | 391210-00-7 | PD318088 (PD-318088), an analog of PD184352, is a novel, potent and non-ATP competitive (allosteric) MEK1/2 inhibitor with potential anticancer activity. |
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V0449 | PD98059 | 167869-21-8 | PD98059 is a novel flavanoid acting as a selective, reversible, andnon-ATP competitive MEK inhibitor with potential anti-inflammatory and anticancer activity. |
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V0455 | Pimasertib (SAR245509, AS703026, MSC1936369B) | 1236699-92-5 | Pimasertib (formerly SAR-245509,AS-703026, MSC-1936369B) is a selective, orally bioavailable and non-ATP competitive (allosteric) inhibitor of MEK1/2 with potential anticancer activity. |
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V0461 | Refametinib (RDEA119, BAY86-9766) | 923032-37-5 | Refametinib (formerly RDEA-119, BAY 86-9766) is an orally bioavailable, highly selective and non-ATP-competitive (allosteric) inhibitor of MEK1/2 with potential antitumor activity. |
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V3658 | Ro 5126766 | 946128-88-7 | Ro 5126766 (also known as Ro-5126766; CH5126766) is a novel, potent, first-in-class dual inhibitor of MEK/RAFmitogen-activated protein kinases (MAPKs) with anticancer activity. |
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V3012 | RO4987655 | 874101-00-5 | PD 169316 is a novel potent, cell-permeable and specific/selective inhibitor of p38 MAPK kinase with IC50 value of 89 nM. |
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V0444 | Selumetinib (AZD-6244; ARRY142886) | 606143-52-6 | Selumetinib (also known as AZD6244; ARRY-142886; Koselugo) is a novel, potent, highly selective and orally bioavailable small molecule MEK1 inhibitor with anticancer activity. |
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V37565 | Selumetinib sulfate (AZD6244 sulfate) | 943332-08-9 | Selumetinib sulfate (also known as AZD6244 sulfate; ARRY-142886 sulfate) is a novel, potent, highly selective, orally bioavailable, andnon-ATP-competitivesmall molecule MEK1 inhibitor with IC50 of 14 nM in cell-free assays and with anticancer activity, it also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. |
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V0456 | SL-327 | 305350-87-2 | SL327 (SL-327) is a novel, potent and selective inhibitor for MEK1/2 with the ability to cross blood brain barrier andblock fear conditioning. |
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V0459 | TAK-733 | 1035555-63-5 | TAK-733 is a novel, potent, selective andorally bioavailable allosteric (non-ATP competitive) inhibitor of MEK with potential anticancer activity. |
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V74085 | Trametiglue | 2666940-97-0 | Trametiglue is an analogue of trametinib that targets KSR-MEK and RAF-MEK with unprecedented potency and selectivity through unique interfacial binding interactions. |
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V0446 | Trametinib (GSK-1120212; JTP-74057; Mekinist) | 871700-17-3 | Mirdametinib (PD-0325901) is a novel, potent, selective, orally bioavailable and non ATP-competitive inhibitor of the mitogen-activated protein kinase MEK with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. |
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V3734 | Trans-Zeatin | 1637-39-4 | Trans-Zeatin is a plant hormone /cytokinin that plays an important role in cell growth, differentiation, and division, it promotes growth of lateral buds, stimulates seed germination and seedling growth, and induces cell division. |
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V4734 | Trans-Zeatin HCl | Trans-Zeatin is a plant hormone /cytokinin that plays an important role in cell growth, differentiation, and division, it promotes growth of lateral buds, stimulates seed germination and seedling growth, and induces cell division. | |
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V2681 | U0126 | 109511-58-2 | U0126 (also known as U0126-EtOH) is a novel potent,highlyselective and non-ATP competitive inhibitor of MEK1/2 with IC50 of 0.07μM/0.06μM in cell-free assays. |
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