KT 5720 | CAS#108068-98-0 | Protein kinase A Inhibitor

MedKoo Cat#: 532045 | Name: KT 5720

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

KT 5720 is a potent, selective inhibitor of protein kinase A (Ki = 60 nM). KT 5720 reversibly arrests human skin fibroblasts in the G1 phase.

Chemical Structure

KT 5720

CAS#108068-98-0

Theoretical Analysis

MedKoo Cat#: 532045

Name: KT 5720

CAS#: 108068-98-0

Chemical Formula: C32H31N3O5

Exact Mass: 537.2264

Molecular Weight: 537.62

Elemental Analysis: C, 71.49; H, 5.81; N, 7.82; O, 14.88

Price and Availability

Size	Price	Availability
100µg	USD 350.00	2 Weeks
250µg	USD 650.00	2 Weeks
500µg	USD 950.00	2 Weeks

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Related CAS #

No Data

Synonym

KT 5720; KT5720; KT-5720.

IUPAC/Chemical Name

hexyl (15R,16R,18S)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8,10,12,20,22,24-nonaene-16-carboxylate

InChi Key

ZHEHVZXPFVXKEY-IKZDWWSZSA-N

InChi Code

InChI=1S/C32H31N3O5/c1-3-4-5-10-15-39-30(37)32(38)16-23-34-21-13-8-6-11-18(21)25-26-20(17-33-29(26)36)24-19-12-7-9-14-22(19)35(28(24)27(25)34)31(32,2)40-23/h6-9,11-14,23,38H,3-5,10,15-17H2,1-2H3,(H,33,36)/t23-,31+,32-/m0/s1

SMILES Code

O=C([C@](C[C@@](O1)([H])N2C3=CC=CC=C43)(O)[C@]1(C)N5C6=CC=CC=C6C7=C5C2=C4C8=C7CNC8=O)OCCCCCC

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 µM).

In vitro activity:

KT-5720 application during EWD (ethanol withdrawal) also restored thionine staining in CA1, suggesting kinase regulation of both neurons and non-neuronal cells. These data demonstrate that CIE (chronic, intermittent ethanol) exposure alters protein kinase activity to promote ethanol withdrawal-associated loss of NeuN/Fox-3 and highlight the influence of kinase signaling on distinct cell types in the developing hippocampus. Reference: Alcohol. 2017 Nov;64:37-43. https://pubmed.ncbi.nlm.nih.gov/28965654/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	13.9	25.93
	Methanol	5.0	9.30

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 537.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Reynolds AR, Saunders MA, Berry JN, Sharrett-Field LJ, Winchester S, Prendergast MA. Broad-spectrum protein kinase inhibition by the staurosporine analog KT-5720 reverses ethanol withdrawal-associated loss of NeuN/Fox-3. Alcohol. 2017 Nov;64:37-43. doi: 10.1016/j.alcohol.2017.05.006. Epub 2017 Aug 30. PMID: 28965654; PMCID: PMC6662204. 2. Cheng Q, Zhou Y. 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. doi: 10.1089/dna.2013.2021. PMID: 23713946; PMCID: PMC3666193.

In vitro protocol:

In vivo protocol:

TBD

1: Galski H, Sivan H, Lazarovici P, Nagler A. 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. PubMed PMID: 16542724. 2: Galski H, Lazarovici P, Gottesman MM, Murakata C, Matsuda Y, Hochman J. KT-5720 reverses multidrug resistance in variant S49 mouse lymphoma cells transduced with the human MDR1 cDNA and in human multidrug-resistant carcinoma cells. Eur J Cancer. 1995;31A(3):380-8. PubMed PMID: 7786606.