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Rp-8-CPT-cAMPS

Catalog No. T38696   CAS 129735-01-9

Rp-8-CPT-cAMPS is a powerful and competitive antagonist of cAMP-induced activation of cAMP-dependent protein kinase (PKA) I and II. Acting as a potent cAMP analog, Rp-8-CPT-cAMPS exhibits a preference for site A of RI over site A of RII. Additionally, it favors site B of RII over site B of RI. This compound effectively inhibits cAMP-dependent PKA activation and demonstrates selectivity in binding to specific sites within the protein kinase.

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Rp-8-CPT-cAMPS Chemical Structure
Rp-8-CPT-cAMPS, CAS 129735-01-9
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Rp-8-CPT-cAMPS is a powerful and competitive antagonist of cAMP-induced activation of cAMP-dependent protein kinase (PKA) I and II. Acting as a potent cAMP analog, Rp-8-CPT-cAMPS exhibits a preference for site A of RI over site A of RII. Additionally, it favors site B of RII over site B of RI. This compound effectively inhibits cAMP-dependent PKA activation and demonstrates selectivity in binding to specific sites within the protein kinase.
In vitro Rp-8-CPT-cAMPS, at a concentration of 100 μM for 15 minutes, inhibits the phosphorylation of VASP by 6-Bnz-cAMP and significantly reduces VASP phosphorylation caused by forskolin and fenoterol. At the same concentration but extended to 30 minutes, it decreases GTP-loading of Rap1 triggered by both 8-pCPT-2'-O-Me-cAMP and 6-Bnz-cAMP. Additionally, it substantially lowers the increase in bradykinin-induced IL-8 release facilitated by PKA activator 6-Bnz-cAMP and Epac activator 8-pCPT-2'-O-Me-cAMP. At a lower concentration of 10 μM, Rp-8-CPT-cAMPS hinders both endothelium-dependent and -independent relaxation caused by venom in pre-contracted rat mesenteric artery rings.
Molecular Weight 487.87
Formula C16H15ClN5O5PS2
CAS No. 129735-01-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Dostmann WR , et, al. Probing the cyclic nucleotide binding sites of cAMP-dependent protein kinases I and II with analogs of adenosine 3',5'-cyclic phosphorothioates. J Biol Chem. 1990 Jun 25;265(18):10484-91. 2. Roscioni SS, et, al. PKA and Epac cooperate to augment bradykinin-induced interleukin-8 release from human airway smooth muscle cells. Respir Res. 2009 Sep 29;10(1):88. 3. Chaisakul J, et, al. In vivo and in vitro cardiovascular effects of Papuan taipan (Oxyuranus scutellatus) venom: Exploring sudden collapse". Toxicol Lett. 2012 Sep 3;213(2):243-8."

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Keywords

Rp-8-CPT-cAMPS 129735-01-9 Rp 8 CPT cAMPS Rp8CPTcAMPS inhibitor inhibit

 

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