2. Stem Cell/Wnt TGF-beta/Smad
  3. PKA
  4. KT5720

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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KT5720

KT5720 Chemical Structure

CAS No. : 108068-98-0

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Based on 3 publication(s) in Google Scholar

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Description

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[1][2][3].

IC50 & Target

IC50: 11 nM (PHK); 300 nM (PDK1); 3.3 µM (PKA)[3].
In Vitro

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.

KT5720 Related Antibodies

Cell Viability Assay[1]

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.
In Vivo

KT5720 (5 mg/kg; i.p.; single daily for 8 days) reverses completely DNR resistance in MDR1 transgenic mice model[1].

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.
Molecular Weight

537.61

Formula

C32H31N3O5
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: ≥99.0%

SDS (418 KB)

COA (255 KB)

Handling Instructions (2659 KB)
References
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KT5720 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KT5720108068-98-0KT 5720KT-5720PKAProtein kinase AMDR1HCNDRGhaematological malignanciesLM1/MDRcancerInhibitorinhibitorinhibit

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