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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.53%
- CAS No.: 108068-98-0
- 화학식: C32H31N3O5
- 분자량:537.61
-
보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) KT5720
More
Biological Activity
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].
?
KT5720 (3 μM) attenuates Ih in freshly isolated rat DRG neurons and slows down HCN channel activation kinetics[2].
?
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.
-
Cell Line:LM1/MDR cells (carrying and expressing a human MDR1 transgene)
-
Concentration:0-8 µM
-
Incubation Time:72 h
-
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.
-
Animal Model:MDR1 transgenic mice model[1].
-
Dosage:5 mg/kg
-
Administration:Intraperitoneal injection; single daily for 8 days
-
Result:Exhibited the leukopenia induced by daunorubicin in the MDR mice was equivalent to that measured in non-MDR mice treated with daunorubicin alone.
Chemical Information
-
CAS No. 108068-98-0
-
Appearance Solid
-
분자량 537.61
-
화학식 C32H31N3O5
-
Color White to off-white
-
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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
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
순도&문서
-
Data Sheet (278 KB)
-
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)
-
Handling Instructions (2659 KB)
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KT5720 Related Classifications
HY-N6789 Related Classifications
Powered by Bioz