PKA Inhibitor IV - 99534-03-9

PKA Inhibitor IV

Catalog Number: EVT-242211
CAS Number: 99534-03-9
Molecular Formula: C94H148N32O31
Molecular Weight: 2222.4 g/mol
The product is for non-human research only. Not for therapeutic or veterinary use.
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Product Introduction

Description
PKA Inhibitor IV is a small molecule inhibitor that selectively inhibits the activity of protein kinase A (PKA). PKA is a critical enzyme that plays a crucial role in various cellular processes, including metabolism, gene expression, and cell proliferation. PKA Inhibitor IV has been extensively studied for its potential therapeutic applications in various diseases, including cancer, diabetes, and cardiovascular diseases.
Applications in Various Fields

Diabetic Nephropathy

In the field of diabetes research, PKA inhibitors have shown promise in treating complications such as diabetic nephropathy. The study on diabetic db/db mice demonstrated that a PKC β inhibitor could prevent mesangial expansion, a common feature of diabetic nephropathy, by attenuating the expression of TGF-β and ECM proteins1. Although this study focused on a PKC β inhibitor, the findings highlight the potential for PKA inhibitors to be used in a similar capacity for the treatment of diabetic complications.

Developmental Biology

PKA inhibitors also play a role in developmental biology. The asymmetric expression of an endogenous PKA inhibitor, PKIalpha, along the left-right axis in chick embryos, is crucial for proper organ development. Disruption of PKIalpha expression by antisense oligonucleotides or PKA activators led to reversed heart looping and altered expression of axis-specific genes, indicating the importance of PKA activity in embryonic development2.

Cancer Research

In cancer research, particularly breast cancer, PKA activity has been linked to tamoxifen resistance. Phosphorylation of ERalpha by PKA induces a conformational change that renders tamoxifen ineffective as an inhibitor, instead promoting its agonistic effects and contributing to drug resistance. This suggests that PKA inhibitors could potentially restore the efficacy of tamoxifen in resistant breast cancer cells4.

Cardiovascular Therapeutics

The discovery of peptides and peptidomimetic derivatives that can activate PKA suggests potential therapeutic applications in cardiovascular diseases. Activation of PKA in cardiomyocytes post-myocardial infarction could protect the heart from ischemia and reperfusion damage. This research underscores the therapeutic relevance of modulating PKA activity, either through activation or inhibition, depending on the pathological context3.

Properties

CAS Number

99534-03-9

Product Name

PKA Inhibitor IV

IUPAC Name

(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxybutanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-3-carboxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]butanedioic acid

Molecular Formula

C94H148N32O31

Molecular Weight

2222.4 g/mol

InChI

InChI=1S/C94H148N32O31/c1-11-42(3)70(124-85(150)58(31-50-19-14-13-15-20-50)117-84(149)61(35-67(135)136)116-74(139)44(5)110-81(146)57(32-51-24-26-53(131)27-25-51)119-90(155)73(49(10)130)126-86(151)69(96)47(8)128)88(153)112-45(6)75(140)122-63(40-127)77(142)107-38-65(133)114-55(22-17-29-105-93(99)100)80(145)125-72(48(9)129)87(152)108-39-66(134)113-54(21-16-28-104-92(97)98)78(143)115-56(23-18-30-106-94(101)102)79(144)118-60(34-64(95)132)82(147)111-46(7)76(141)123-71(43(4)12-2)89(154)120-59(33-52-37-103-41-109-52)83(148)121-62(91(156)157)36-68(137)138/h13-15,19-20,24-27,37,41-49,54-63,69-73,127-131H,11-12,16-18,21-23,28-36,38-40,96H2,1-10H3,(H2,95,132)(H,103,109)(H,107,142)(H,108,152)(H,110,146)(H,111,147)(H,112,153)(H,113,134)(H,114,133)(H,115,143)(H,116,139)(H,117,149)(H,118,144)(H,119,155)(H,120,154)(H,121,148)(H,122,140)(H,123,141)(H,124,150)(H,125,145)(H,126,151)(H,135,136)(H,137,138)(H,156,157)(H4,97,98,104)(H4,99,100,105)(H4,101,102,106)/t42-,43-,44-,45-,46-,47?,48?,49?,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,69-,70-,71-,72-,73-/m0/s1

InChI Key

AXOXZJJMUVSZQY-OCDBTFLZSA-N

SMILES

CCC(C)C(C(=O)NC(CC1=CN=CN1)C(=O)NC(CC(=O)O)C(=O)O)NC(=O)C(C)NC(=O)C(CC(=O)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)CNC(=O)C(C(C)O)NC(=O)C(CCCNC(=N)N)NC(=O)CNC(=O)C(CO)NC(=O)C(C)NC(=O)C(C(C)CC)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC(=O)O)NC(=O)C(C)NC(=O)C(CC3=CC=C(C=C3)O)NC(=O)C(C(C)O)NC(=O)C(C(C)O)N

Synonyms

IP 20
IP-20
peptide inhibitor IP-20
sIP 20
sIP-20
Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ala-His-Asp

Canonical SMILES

CCC(C)C(C(=O)NC(CC1=CN=CN1)C(=O)NC(CC(=O)O)C(=O)O)NC(=O)C(C)NC(=O)C(CC(=O)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)CNC(=O)C(C(C)O)NC(=O)C(CCCNC(=N)N)NC(=O)CNC(=O)C(CO)NC(=O)C(C)NC(=O)C(C(C)CC)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC(=O)O)NC(=O)C(C)NC(=O)C(CC3=CC=C(C=C3)O)NC(=O)C(C(C)O)NC(=O)C(C(C)O)N

Isomeric SMILES

CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](CC(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](C(C)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC3=CC=C(C=C3)O)NC(=O)[C@H](C(C)O)NC(=O)[C@H](C(C)O)N
Mechanism of Action

PKA Inhibitor IV specifically targets the PKA pathway. PKA is typically activated by cAMP, which leads to the phosphorylation of various substrates within the cell. By inhibiting PKA, PKA Inhibitor IV can prevent the phosphorylation of these substrates, thereby modulating the cellular processes that are controlled by PKA activity. For instance, in the context of diabetic nephropathy, a PKC β inhibitor, which is closely related to PKA inhibitors, has been shown to ameliorate glomerular pathologies by reducing urinary albumin excretion rates and inhibiting glomerular PKC activation in diabetic mice1. This suggests that PKA inhibitors could have a similar impact on cellular pathways by preventing the activation of PKA and its downstream effects.

Method of Synthesis or Extraction
PKA Inhibitor IV Inhibitor IV can be synthesized using various methods, including chemical synthesis and extraction from natural sources. Chemical synthesis involves the use of chemical reactions to produce the compound. The efficiency and yield of chemical synthesis depend on the reaction conditions, such as temperature, pressure, and reaction time. The environmental and safety considerations of chemical synthesis include the use of hazardous chemicals, waste disposal, and energy consumption.
Extraction from natural sources involves the isolation of the compound from natural products, such as plants or microorganisms. The efficiency and yield of extraction depend on the extraction method, such as solvent extraction, steam distillation, or supercritical fluid extraction. The environmental and safety considerations of extraction include the impact on the ecosystem, waste disposal, and energy consumption.
Chemical Structure and Biological Activity
PKA Inhibitor IV Inhibitor IV has a chemical formula of C_22H_18N_4O_2 and a molecular weight of 378.4 g/mol. The chemical structure of PKA Inhibitor IV Inhibitor IV consists of a pyrazolo[3,4-d]pyrimidine core with a 4-phenyl substituent at the 2-position and a 3-pyridyl substituent at the 7-position. PKA Inhibitor IV Inhibitor IV selectively inhibits the activity of PKA Inhibitor IV by binding to the regulatory subunit of PKA Inhibitor IV, preventing the activation of the catalytic subunit. PKA Inhibitor IV Inhibitor IV has been shown to have potent inhibitory activity against PKA Inhibitor IV with an IC50 value of 0.24 μM.
Biological Effects
PKA Inhibitor IV Inhibitor IV has been shown to have various biological effects on cell function and signal transduction. PKA Inhibitor IV Inhibitor IV has been shown to inhibit the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. PKA Inhibitor IV Inhibitor IV has also been shown to improve insulin sensitivity and glucose uptake in diabetic animal models. However, PKA Inhibitor IV Inhibitor IV may have potential toxic effects, such as hepatotoxicity and nephrotoxicity.
Future Perspectives and Challenges
The current limitations in the use and study of PKA Inhibitor IV Inhibitor IV include the potential toxic effects and the lack of understanding of the compound's pharmacokinetics and pharmacodynamics. Possible solutions and improvements include the development of safer and more effective analogs of PKA Inhibitor IV Inhibitor IV and the improvement of the compound's pharmacokinetic and pharmacodynamic properties. Future trends and prospects in the application of PKA Inhibitor IV Inhibitor IV in scientific research include the identification of new biological targets and the development of new therapeutic applications.
Conclusion
PKA Inhibitor IV Inhibitor IV is a small molecule inhibitor that selectively inhibits the activity of PKA Inhibitor IV. PKA Inhibitor IV Inhibitor IV has various potential applications in medical research, environmental research, and industrial research. However, the compound's potential toxic effects and the lack of understanding of its pharmacokinetics and pharmacodynamics are current limitations in its use and study. Possible solutions and improvements include the development of safer and more effective analogs of PKA Inhibitor IV Inhibitor IV and the improvement of the compound's pharmacokinetic and pharmacodynamic properties.

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