KT5823

SKU
K-1040
  • CAS:126643-37-6
  • Formula:C29H25N3O5
  • MW:495.5 Da
  • Appearance:White solid
  • Purity:≥98%

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Product Name Qty
KT-5823
500 ug
$489.99
KT-5823
1 mg
$919.99
KT-5823
100 ug
$139.99

Description

KT5823 is a gamma-lactam protein kinase inhibitor that acts on cGMP-dependent kinase activity. KT5823 inhibits cGMP-dependent kinase activity only in an in vitro context and has never been demonstrated to exert the same inhibitory effect in vivo. Indeed, one prominent study of the effects of KT5823 in both intact human and rat cells suggests that the inhibitory effect of this kinase inhibitor may be confined to the in vitro domain.

 

Applications

Despite its apparent lack of in vivo activity, KT5823 has been used widely in biomedical research to establish the role of cGMP-dependent kinase activity in various cellular processes. It has also been used as a reagent in pharmacological research pertaining to hormone-induced NIS expression

• Staurosporine-related protein kinase inhibitor
in vitro inhibitor of cGK
• Inhibits cGMP-dependent protein kinase activity in vitro but not in intact human platelets and rat mesangial cells
• Shown to increase thyroid-stimulating hormone-induced Na+/I- symporter expression, and thus iodide uptake in thyroid cells
• KT5823-mediated effects on Na+/I- symporter activity and glycosylation are also observed in breast cancer cells as well as human embryonic kidney cells expressing exogenous NIS

 

More Information
Alternate Name/Synonyms
AC1L1GU8; CTK8E8623; KS-0000182G; RT-013452; J-005415
SKU
K-1040
CAS #
126643-37-6
Chemical Name
methyl (15S,16R,18R)-16-methoxy-4,15-dimethyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate
Chemical Formula
C29H25N3O5
Molecular Weight
495.5 Da
Appearance
White solid
Purity
≥98%
Solubility
DMSO @ 25 mg/mL, DMF @ 20 mg/mL, EtOAc @ 5 mg/mL
Melting Point
272 - 276°C
Preparation
N/A
Storage Temp
+4°C
THERAPEUTIC AREA
Not Available
USE
For laboratory and research purpose only. KT5823 is a derivative of K-252a (sc-200517) and a selective inhibitor of cGMP-dependent protein kinases (cGKI, Ki=2.4nM) in vitro, but does not inhibit cGMP-dependent protein kinase phosphorylation of VASP in either intact platelets or rat mesangial cells. KT5823 has also been shown to dose-dependently inhibit spontaneous apoptosis of neutrophils, thus suggesting cGK as a mediator of neutrophil spontaneous apoptosis.
Merck Index
N/A
RTECS
N/A
Handling
Ensure adequate ventilation, especially in confined areas. Use personal protective equipment as required. Use with local exhaust ventilation. Avoid inhalation of any substances.
Certificate of Analysis 1
Certificate of Analysis 2
Certificate of Analysis 3
GHS PICTOGRAMS
Handling Ensure adequate ventilation, especially in confined areas. Use personal protective equipment as required. Use with local exhaust ventilation. Avoid inhalation of any substances.
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