KT5720
Based on 4 publication(s) in Google Scholar
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2+ concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases.
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- 純度: 98.53%
- CAS 番号: 108068-98-0
- 分子式: C32H31N3O5
- 分子量:537.61
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
IC50: 11 nM (PHK); 300 nM (PDK1); 3.3 µM (PKA)[3].
KT5720 (0-8 μM; 72 h) reverses multidrug resistance in an MDR1 lymphoma cell model[1].
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KT5720 (3 μM) attenuates Ih in freshly isolated rat DRG neurons and slows down HCN channel activation kinetics[2].
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KT5720 (3 μM) reduces DRG neurons excitability and reduces DRG neuron intracellular Ca2 + level[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LM1/MDR cells (carrying and expressing a human MDR1 transgene)
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Concentration:0-8 µM
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Incubation Time:72 h
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Result:Increased sensitivity of LM1/MDR cells to colchicine in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDR1 transgenic mice model[1].
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; single daily for 8 days
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Result:Exhibited the leukopenia induced by daunorubicin in the MDR mice was equivalent to that measured in non-MDR mice treated with daunorubicin alone.
化学情報
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CAS 番号 108068-98-0
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性状 Solid
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分子量 537.61
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分子式 C32H31N3O5
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Color White to off-white
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SMILES
C[C@@]12N3C4=C(C5=CC=CC=C35)C(CNC6=O)=C6C7=C4N(C8=CC=CC=C87)[C@@](C[C@@]2(O)C(OCCCCCC)=O)([H])O1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Metab
The thermogenic activity of adjacent adipocytes fuels the progression of ccRCC and compromises anti-tumor therapeutic efficacy. [Abstract]2021 Oct 5;33(10):2021-2039.e8. PMID: 34508696 -
Cell Metab
The phytochemical hyperforin triggers thermogenesis in adipose tissue via a Dlat-AMPK signaling axis to curb obesity. [Abstract]2021 Mar 2;33(3):565-580.e7. PMID: 33657393 -
Oncogene
FBXO28 suppresses liver cancer invasion and metastasis by promoting PKA-dependent SNAI2 degradation. [Abstract]2023 Sep;42(39):2878-2891. PMID: 37596321 -
Int J Biochem Cell Biol
Downregulation of Pannexin-1 attenuates sepsis-induced acute lung injury via activation of the cAMP/PKA pathway. [Abstract]2026 Jun-Jul:195-196:106941. PMID: 41850417
純度とドキュメンテーション
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データシート (278 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Galski H, et al. In vitro and in vivo reversal of MDR1-mediated multidrug resistance by KT-5720: implications on hematological malignancies. Leuk Res. 2006 Sep;30(9):1151-8. [Content Brief]
[2]. Cheng Q, et al. Novel role of KT5720 on regulating hyperpolarization-activated cyclic nucleotide-gated channel activity and dorsal root ganglion neuron excitability. DNA Cell Biol. 2013 Jun;32(6):320-8. [Content Brief]
[3]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
KT5720 関連分類
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