A LIMK1 inhibitor
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SR 7826

Item No. 32976

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2-hydroxyethyl)-N′-[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]-N-phenyl-urea
CAS Number
1219728-20-7
Molecular Formula
C22H21N5O2
Formula Weight
387.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O=C(N(CCO)C1=CC=CC=C1)NC2=CC=C(C3=C4C(C)=CNC4=NC=N3)C=C2
InChi Code
InChI=1S/C22H21N5O2/c1-15-13-23-21-19(15)20(24-14-25-21)16-7-9-17(10-8-16)26-22(29)27(11-12-28)18-5-3-2-4-6-18/h2-10,13-14,28H,11-12H2,1H3,(H,26,29)(H,23,24,25)
InChi Key
WQAGVQVBDHOHRD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $164

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    10 mg

    $295

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    25 mg

    $575

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    50 mg

    $984

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    Product Description

    SR 7826 is an inhibitor of LIM kinase 1 (LIMK1; IC50 = 43 nM).1 It is selective for LIMK1 over Rho-associated kinase 1 (ROCK1) and ROCK2 (IC50s = 6,565 and 5,536 nM, respectively) and a panel of 60 kinases at 1 µM but does inhibit serine/threonine kinase 16 (STK16) by greater than 80% at 1 µM. SR 7826 inhibits the phosphorylation of cofilin induced by hepatocyte growth factor (HGF) in A7r5 cells (IC50 = 470 nM). It reduces the migration and invasion of PC3 prostate cancer cells when used at a concentration of 1 µM. SR 7826 (1 µM) inhibits electric field stimulation-, phenylephrine-, methoxamine-, norepinephrine-, or U-46619-induced contractions of prostate strips isolated from patients with prostate cancer.2 In vivo, SR 7826 (10 mg/kg, p.o.) increases apical and basal thin spine density of CA1 pyramidal neurons in the hAPP-J20 mouse model of Alzheimer’s disease.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yin, Y., Zheng, K., Eid, N., et al. Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors. J. Med. Chem. 58(4), 1846-1861 (2015).

    2. Yu, Q., Gratzke, C., Wang, Y., et al. Inhibition of human prostate smooth muscle contraction by the LIM kinase inhibitors, SR7826 and LIMKi3. Br. J. Pharmacol. 175(11), 2077-2096 (2018).

    3. Henderson, B.W., Greathouse, K., Ramdas, R., et al. Pharmacologic inhibition of LIMK1 provides dendritic spine resilience against β-amyloid. Sci. Signal 12(587), eaaw9318 (2019).