1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK
  3. ERK-IN-2

ERK-IN-2 

Cat. No.: HY-133084
Handling Instructions

ERK-IN-2 is a potent, highly seletive and orally active 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.

For research use only. We do not sell to patients.

ERK-IN-2 Chemical Structure

ERK-IN-2 Chemical Structure

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Description

ERK-IN-2 is a potent, highly seletive and orally active 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[1].

IC50 & Target[1]

ERK2

1.8 nM (IC50)

In Vitro

ERK-IN-2 (1 μM) has effects on cell proliferation with IC50 values of 214 nM; 305 nM; 91 nM and 201 nM for A375SM cell, SK-MEL 30 cell; Colo 205 cell and Lovo cell, respectively[1].

In Vivo

ERK-IN-2 (1 mpk/oral 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[1].

Molecular Weight

347.80

Formula

C₁₆H₁₈ClN₅O₂

SMILES

OCC1=NC(NC(N[[email protected]](C)C2=CC=CC=C2)=O)=CC3=C1C=NN3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

ERK-IN-2ERKExtracellular signal regulated kinasescancerMRK-ERKiInhibitorinhibitorinhibit

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ERK-IN-2
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