ERK-IN-2 is a ERK2 inhibitor probe with an IC50 value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM.
Molecular Weight: 347.80
Chemical Name: 3-[4-(hydroxymethyl)-1H-pyrazolo[4,3-c]pyridin-6-yl]-1-[(1R)-1-phenylethyl]urea hydrochloride
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
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
How to use
The criteria of inhibitor probe: Inhibitor potency: goal is <100 nM (IC50); Selectively with target family: >30-fold. We recommend ERK-IN-2 (MRK-ERKi) to be used at a concentration of 1 μM in cell-based experiments and do not recommend doses >10 μM to be employed in any experiment. ERK-IN-2 (1 μM) has effects on cell proliferation in cancer cell lines. The IC50 values are 214 nM; 305 nM; 91 nM and 201 nM for A375SM cell, SK-MEL 30 cell; Colo 205 cell and Lovo cell, respectively.
ERK-IN-2 (1 mpk; orally administation/0.5 mpk; intravenous injection) shows a DMPK value: h/r/d LM CLint: <17/235/<75 (mL/min/kg); uCLp:217 mL/min/kg; uVd 5.7 L/kg; t1/2: 0.4 h; rat F:13% in SD rat.
- MRK-ERK Inhibitor and Negative Control
Products are for research use only. Not for human use.
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