1. MAPK/ERK Pathway
    Apoptosis
  2. MEK
    Apoptosis
  3. PD184161

PD184161 

Cat. No.: HY-10174
Handling Instructions

PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior.

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

PD184161 Chemical Structure

PD184161 Chemical Structure

CAS No. : 212631-67-9

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5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
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Description

PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior[1][2].

IC50 & Target[1]

MEK

10-100 nM (IC50)

In Vitro

PD184161 (1-20 μM; 24, 48, or 72 hours) inhibits cell proliferation and induces apoptosis in a time and concentration dependent manner[1].
PD184161 (0.1 and 1.0 μM; 1 hour) inhibits ERK1,2 phosphorylation[1].
PD184161 (5 μM; 30 min) prevents the toxic effects of bicuculline[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
Concentration: 1-20 μM
Incubation Time: 24, 48, or 72 hours
Result: Inhibited cell proliferation.

Apoptosis Analysis[1]

Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
Concentration: 1-20 μM
Incubation Time: 48 hours
Result: Induced cell apoptosis.

Western Blot Analysis[1]

Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
Concentration: 0.1 and 1.0 μM
Incubation Time: 1 hours
Result: Inhibited ERK1,2 phosphorylation.

Cell Viability Assay[3]

Cell Line: Primary mouse neurons
Concentration: 5 μM
Incubation Time: 30 min
Result: Prevents the toxic effects of bicuculline.
In Vivo

PD184161 reduces tumor xenograft P-ERK levels in 3-12 hours after an oral dose[1].
PD184161 (300 mg/kg; orogastric gavage twice daily for 38 days) significantly suppresses tumor engraftment and initial growth[1].
PD184161 (30 mg/kg; i.p.; single injection) produces depressive-like behavior[2].
PD184161 (500 μg/kg; intravenous injection) prevents the progression of neurological deficits and brain damage after stroke[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Hep3B tumor xenografts BALB/c athymic nude mice[1]
Dosage: 300 mg/kg
Administration: Orogastric gavage twice daily for 38 days
Result: Decreased the early tumor growth.
Animal Model: Male, 6 weeks C57Bl/6 mice[2]
Dosage: 500 μg/kg
Administration: intravenously in 30 min before MCAO or PTZ administration
Result: Prevented the progression of neurological deficits and brain damage after stroke.
Animal Model: C57Bl/6 mice[3]
Dosage: 30 mg/kg
Administration: i.p., single injection
Result: Produced depressive-like behavior.
Molecular Weight

557.56

Formula

C₁₇H₁₃BrClF₂IN₂O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

References
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PD184161
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