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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 |
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Molecular Formula | C29H25N3O5 |
CAS No. | 126643-37-6 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 10mM |
Water: N/A | |
Ethanol: N/A | |
SMILES Code | O=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 |
Synonyms | KT-5823; KT5823; KT 5823 |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.0180 mL | 10.0900 mL | 20.1800 mL | 40.3600 mL |
5mM | 0.4036 mL | 2.0180 mL | 4.0360 mL | 8.0720 mL |
10mM | 0.2018 mL | 1.0090 mL | 2.0180 mL | 4.0360 mL |
20mM | 0.1009 mL | 0.5045 mL | 1.0090 mL | 2.0180 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.