ERK
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S7101 | SCH772984 | <1 mg/mL | 14 mg/mL | <1 mg/mL |
| S7921 | DEL-22379 | <1 mg/mL | 89 mg/mL | <1 mg/mL |
| S7709 | VX-11e | <1 mg/mL | 100 mg/mL | 16 mg/mL |
| S7334 | ERK5-IN-1 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7525 | XMD8-92 | <1 mg/mL | 73 mg/mL | <1 mg/mL |
| S8534 | LY3214996 | <1 mg/mL | 27 mg/mL | 16 mg/mL |
| S7752 | Pluripotin (SC1) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7854 | Ulixertinib (BVD-523, VRT752271) | <1 mg/mL | 86 mg/mL | 15 mg/mL |
| S7524 | FR 180204 | <1 mg/mL | 65 mg/mL | 2 mg/mL |
| S7554 | GDC-0994 | <1 mg/mL | 87 mg/mL | 87 mg/mL |
Isoform-specific Inhibitors
- ERK Inhibitors (10)
- New ERK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7101 |
SCH772984SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells. |
293T cells were transfected with Flag-WT-FBW7. Thirty hours post transfection, cells were pretreated with MG132 and various MEK/ERK inhibitors overnight before harvesting. FBW7 phosphorylation status was examined by immunoblot analysis after immunoprecipitation.
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| S7921 |
DEL-22379DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM. |
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| S7709 |
VX-11eVX-11e is a potent, selective, and orally bioavailable ERK2 inhibitor with Ki of <2 nM, over 200-fold selective over other kinases tested. |
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| S7334 |
ERK5-IN-1ERK5-IN-1 is a potent, and selective ERK5 inhibitor with IC50 of 162 nM. |
The effect of ERK5-IN-1 on botrocetin/VWF-induced human platelet two-wave aggregation.
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| S7525 |
XMD8-92XMD8-92 is a potent and selective BMK1/ERK5 inhibitor with Kd of 80 nM. |
Representative images (20x magnification, scale bar 100 μm) of tumor histology (H&E and trichrome staining) and IHC staining for DNA double strand breaks (DSBs, γH2AX staining) from control and Hsp90i+Erk5i treated mice on day 13.
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| S8534New |
LY3214996LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. |
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| S7752 |
Pluripotin (SC1)Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP with Kd values of 98 nM and 212 nM respectively. It maintains embryonic stem cell (ESC) self-renewal. |
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| S7854 |
Ulixertinib (BVD-523, VRT752271)Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1. |
Ulixertinib inhibited the proliferation of SUDHL-10 and Raji cells. (A) The activation of ERK1/2 was analyzed by Western blotting. Ulixertinib (0.1, 0.4 and 1.0 nM) significantly inhibited ERK1/2 activation in a dose-dependent manner compared with control cells. Cell proliferation was measured by the CCK-8 assay. Ulixertinib (0.1, 0.4 and 1.0 nM) significantly inhibited proliferation of SUDHL-10 (B) and Raji cells (C) in a time- and dose-dependent manner compared with control cells.
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| S7524 |
FR 180204FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively. It is 30-fold less potent against the related kinase p38α and failed to inhibit any kinases(MEK1, MKK4, IKKα, PKCα, Src, Syc, and PDGFα) at less than 30 μM. |
ERK1/2 inhibition reverse EMT in H1299- EML4-ALK cells. H1299-EML4-ALK cells were treated with FR180204 (10 μM), crizotinib (10 nM) and S3I-201(20 μM) for 24 h, cell extracts were analyzed by immunoblotting.
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| S7554 |
GDC-0994GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1. |
Pancreatic acini exposed for 1 h to 300 μM of oleic acid (OA) or linoleic acid (LA) were pre-treated for 45 min with the vehicle (DMSO) or SP600125 (50 μM), GDC-0994 (50 μM) or SB202190 (50 μM) or AG-490 (50 μM) respectively. CCL2mRNA expression was analyzed by qRT-PCR with 18S as internal standard. *p<0.05, **p<0.01 as compared with untreated acini, ♦♦p<0.01 as compared with OA- or LA-treated acini.
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