ERK5-IN-1

Catalog No.S7334 Batch:S733401

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Technical Data

Formula

C36H46N8O3

Molecular Weight 638.81 CAS No. 1435488-37-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (156.54 mM)
Ethanol 100 mg/mL (156.54 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description ERK5-IN-1 (XMD17-109) is a potent, and selective ERK5 inhibitor with IC50 of 162 nM.
Targets
ERK5 [1]
162 nM
In vitro ERK5-IN-1 potently inhibits ERK5 biochemically with an IC50 of 162 nM and in cells with a cellular EC50 for inhibiting epidermal growth factor induced ERK5 autophosphorylation of 0.09 μM.[1]

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , J Thromb Haemost, 2017, 15(8):1679-1688]

Selleck's ERK5-IN-1 has been cited by 7 publications

NKX2-5 regulates vessel remodeling in scleroderma-associated pulmonary arterial hypertension [ JCI Insight, 2024, 9(10)e164191] PubMed: 38652537
Transcriptional control of pancreatic cancer immunosuppression by metabolic enzyme CD73 in a tumor-autonomous and -autocrine manner [ Nat Commun, 2023, 14(1):3364] PubMed: 37291128
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors [ J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096] PubMed: 34710325
Reversal of ABCB1-related multidrug resistance by ERK5-IN-1. [ J Exp Clin Cancer Res, 2020, 12;39(1):50] PubMed: 32164732
Aurora kinase inhibition sensitizes melanoma cells to T-cell-mediated cytotoxicity [ Cancer Immunol Immunother, 2020, 10.1007/s00262-020-02748-9] PubMed: 33123754
Increased Expression of EGR1 and KLF4 by Polysulfide via Activation of the ERK1/2 and ERK5 Pathways in Cultured Intestinal Epithelial Cells [ Biomed Res, 2020, 41(3):119-129] PubMed: 32522929
Extracellular signal-regulated kinase 5 associates with casein kinase II to regulate GPIb-IX-mediated platelet activation via the PTEN/PI3K/Akt pathway [ J Thromb Haemost, 2017, 15(8):1679-1688] PubMed: 28603902

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.