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Chemical Structure| 2095432-71-4 Chemical Structure| 2095432-71-4

Structure of GSK269962A HCl
CAS No.: 2095432-71-4

Chemical Structure| 2095432-71-4

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GSK269962 HCl is a selective ROCK (Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

Synonyms: GSK269962 hydrochloride; GSK269962B; GSK269962

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Product Details of GSK269962A HCl

CAS No. :2095432-71-4
Formula : C29H31ClN8O5
M.W : 607.06
SMILES Code : O=C(NC1=CC=CC(OC2=CC3=C(N=C(C4=NON=C4N)N3CC)C=N2)=C1)C5=CC=C(OCCN6CCOCC6)C=C5.[H]Cl
Synonyms :
GSK269962 hydrochloride; GSK269962B; GSK269962
MDL No. :MFCD31536773
InChI Key :UYKVMFKKKLLDGL-UHFFFAOYSA-N
Pubchem ID :57398146

Safety of GSK269962A HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of GSK269962A HCl

cytoskeleton

Isoform Comparison

Biological Activity

Description
GSK269962A (GSK 269962) is a potent ROCK inhibitor, which effective against both ROCK1 and ROCK2 isoforms, with IC50 values of 1.6 and 4 nM, respectively. GSK269962A has anti-inflammatory and vasodilatory activities[1].
Target
  • ROCK1

    ROCK1, IC50:1.6 nM

  • ROCK2

    ROCK2, IC50:4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
OCI-AML3 80 nM 72 hours CGM097 showed synergy with AZD6244 in OCI-AML3 cells PMC9763303
MV4-11 80 nM 72 hours To evaluate the effect of PLX51107 on AML cell viability, results showed that PLX51107 reduced AML cell viability PMC9763303
LepR+ MSCs 1 μM 48 hours Inhibition of ROCK1 signaling pathway, reducing the expression of fibrosis markers Col1a1, vimentin, and α-SMA PMC11071275
UACC62 625nM 48 hours To evaluate the effect of GSK269962A on the proliferation of MAPKi-resistant melanoma cells, showing complete inhibition of proliferation at 625nM concentration. PMC10802590
M481 625nM 48 hours To evaluate the effect of GSK269962A on the proliferation of MAPKi-resistant melanoma cells, showing complete inhibition of proliferation at 625nM concentration. PMC10802590
A375 625nM 48 hours Evaluate the effect of XL888 on the viability of A375 cells, results showed that XL888 did not significantly reduce cell viability. PMC10802590

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD-SCID/IL2Rgnull mice AML model 5 mg/kg and 10 mg/kg Intraperitoneal injection 5 days per week for 4 weeks Significantly prolonged mouse survival and reduced leukemia cell infiltration PMC9763303
Mice PE-induced prostatic hyperplasia model 5 mg/kg Intraperitoneal injection Four times a week for four weeks GSK269962A reduces prostatic stromal hyperplasia and collagen deposition by inhibiting ROCK1 signaling pathway PMC11071275

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.65mL

0.33mL

0.16mL

8.24mL

1.65mL

0.82mL

16.47mL

3.29mL

1.65mL

References

 

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