KT5823

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KT5823
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Cat #: V4102 CAS #: 126643-37-6 Purity ≥ 98%

Description: KT5823 (KT-5823), a staurosporine-related analog, is a selective inhibitor of protein kinase G (PKG) with anticancer activity. It inhibits protein kinases with Ki values of 0.23, 4 and > 10 μM for PKG, PKC and PKA respectively. KT5823 has been shown to increase thyroid-stimulating hormone-induced NIS expression, and thus iodide uptake, in thyroid cells. In this study, we found that KT5823 does not increase but decreases iodide uptake within 0.5 h of treatment in trans-retinoic acid and hydrocortisone-treated MCF-7 breast cancer cells. Moreover, KT5823 accumulates hypoglycosylated NIS, and this effect is much more evident in breast cancer cells than thyroid cells. The hypoglycosylated NIS is core glycosylated, has not been processed through the Golgi apparatus, but is capable of trafficking to the cell surface. KT5823 impedes complex NIS glycosylation at a regulatory point similar to brefeldin A along the N-linked glycosylation pathway, rather than targeting a specific N-glycosylated site of NIS. KT5823-mediated effects on NIS activity and glycosylation are also observed in other breast cancer cells as well as human embryonic kidney cells expressing exogenous NIS. Taken together, KT5823 will serve as a valuable pharmacological reagent to uncover mechanisms underlying differential NIS regulation between thyroid and breast cancer cells at multiple levels.

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Molecular Weight (MW)495.54
Molecular FormulaC29H25N3O5
CAS No.126643-37-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 10mM
Water: N/A
Ethanol: N/A
SMILES CodeO=C([C@](C[C@](O1)([H])N2C3=CC=CC=C43)(OC)[C@@]1(C)N5C6=CC=CC=C6C7=C5C2=C4C8 =C7CN(C)C8=O)OC
SynonymsKT-5823; KT5823; KT 5823
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.0180 mL10.0900 mL20.1800 mL40.3600 mL
5mM0.4036 mL2.0180 mL4.0360 mL8.0720 mL
10mM0.2018 mL1.0090 mL2.0180 mL4.0360 mL
20mM0.1009 mL0.5045 mL1.0090 mL2.0180 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.