1. Cell Cycle/DNA Damage
  2. LIM Kinase (LIMK)
  3. SR7826

SR7826 

Cat. No.: HY-19353
Handling Instructions

SR7826 is a class of bis-aryl urea derived potent, selective and orally active LIM kinase (LIMK) inhibitor with an IC50 of 43 nM for LIMK1. SR7826 is >100-fold more selective for LIMK1 than ROCK and JNK kinases.

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

SR7826 Chemical Structure

SR7826 Chemical Structure

CAS No. : 1219728-20-7

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Description

SR7826 is a class of bis-aryl urea derived potent, selective and orally active LIM kinase (LIMK) inhibitor with an IC50 of 43 nM for LIMK1. SR7826 is >100-fold more selective for LIMK1 than ROCK and JNK kinases[1].

IC50 & Target[1]

LIMK1

43 nM (IC50)

ROCKI

5536 nM (IC50)

ROCKII

6565 nM (IC50)

In Vitro

In the profiling against a panel of 61 kinases, SR7826 (compound 18b) at 1 μM inhibits only Limk1 and STK16 with ≥80% inhibition. SR7826 is highly efficient in inhibiting cell-invasion/migration in PC-3 cells. SR7826 (compound 18b) inhibits cofilin phosphorylation in A7r5 (IC50 = 470 nM) and PC-3 cells (IC50 < 1 µM)[1].
SR7826 (1 μM) inhibits contractions of prostate strips, which were induced by electrical field stimulation and inhibits cofilin phosphorylation in prostate tissues and cultured stromal cells (WPMY-1). In WPMY-1 cells, SR7826 causes breakdown of actin filaments and reduced viability[3].

In Vivo

SR7826 (10 mg/kg; oral gavage; once daily; for 11 days; hAPPJ20 mice) treatment significantly reduces the phosphorylation of cofilin at Ser3. SR7826 also increases both apical and basal thin spine density significantly in hAPPJ20 mice over mock-treated animals[2].
The plasma pharmacokinetics studies on rats are investigated. After intravenous injection, the PK properties of SR7826 (compound 18b; 1mg/kg) with a Cl of 5.2 mL/min/kg, a T1/2 of 2.2h, an AUC of 8.4 μM*h and a Cmax of 7.7 μM, and has 36% oral bioavailability in rats (oral administration; 2mg/kg)[1].

Animal Model: hAPPJ20 mice (6-mouth-old)[2]
Dosage: 10 mg/kg
Administration: Oral gavage; once daily; for 11 days
Result: Significantly reduced the phosphorylation of cofilin at Ser3, a LIMK1 substrate.
Molecular Weight

387.43

Formula

C₂₂H₂₁N₅O₂

CAS No.

1219728-20-7

SMILES

O=C(NC1=CC=C(C2=C3C(NC=C3C)=NC=N2)C=C1)N(CCO)C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

SR7826SR 7826SR-7826LIM Kinase (LIMK)LIMKsLimk1STK16bis-arylureascofilinphosphorylationinvasionmigrationpharmacokineticsInhibitorinhibitorinhibit

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SR7826
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