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AB143787

H-89, PKA inhibitor

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(8 Publications)

MW 519.3 Da, Purity >98%. Kinase inhibitor, commonly used as a protein kinase A inhibitor (IC50 = 135 nM). Also inhibits other kinases, including MSK1 , S6K1 and ROCKII (IC50 values are 120, 80 and 270 nM, respectively).

View Alternative Names

AKT, AKT2_HUMAN, AKT3 kinase, AKT3_HUMAN, DKFZp434N0250, HIHGHH, KAPCA_HUMAN, KIAA0619, MPPH, Oncogene AKT2 protein kinase B beta, PKA C-alpha, PKA C-beta, PKACA, PKACB, PKB, PKB beta, PKB-GAMMA, PKBB, PKBG, PPNAD4, PRKACA, PRKACAA, PRKACB, PRKBB, PRKBG, Protein kinase A catalytic subunit, Protein kinase A catalytic subunit alpha, Protein kinase A catalytic subunit beta, Protein kinase Akt-2, Protein kinase Akt-3, Protein kinase B beta, Protein kinase B gamma, Protein kinase cAMP dependent catalytic beta, Protein kinase, cAMP dependent, catalytic, alpha, RAC-BETA, RAC-PK-beta, RAC-PK-gamma, RAC-beta serine/threonine-protein kinase, RAC-gamma, RAC-gamma serine/threonine-protein kinase, ROCK2_HUMAN, ROK alpha, Rho associated coiled coil containing protein kinase 2, Rho associated, coiled coil containing protein kinase II, Rho kinase 2, Rho-associated, Rho-associated protein kinase 2, Rock II, Rock2m, STK-2, Serine threonine protein kinase Akt 3, V akt murine thymoma viral oncogene homolog 3 (protein kinase B, gamma), V akt murine thymoma viral oncogene homolog 3 protein kinase B gamma, V-AKT murine thymoma viral oncogene homolog 2, V-AKT murine thymoma viral oncogene homolog 3, cAMP dependent protein kinase alpha catalytic subunit, cAMP dependent protein kinase beta catalytic subunit, cAMP dependent protein kinase catalytic subunit alpha, isoform 1, cAMP-dependent protein kinase catalytic beta subunit isoform 4ab, cAMP-dependent protein kinase catalytic subunit alpha, cAMP-dependent protein kinase catalytic subunit beta, coiled-coil-containing protein kinase 2, murine thymoma viral (v-akt) homolog-2, p164 ROCK-2, rac protein kinase beta

1 Images
Chemical Structure - H-89, PKA inhibitor (AB143787)
  • Chemical Structure

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Chemical Structure - H-89, PKA inhibitor (AB143787)

2D chemical structure image of ab143787, H-89, PKA inhibitor

Key facts

CAS number

130964-39-5

Purity

>98%

Form

Solid

form

Molecular weight

519.3 Da

Molecular formula

C<sub>2</sub><sub>0</sub>H<sub>2</sub><sub>2</sub>BrCl<sub>2</sub>N<sub>3</sub>O<sub>2</sub>S

PubChem

5702541

Nature

Synthetic

Biochemical name

H-89 Dihydrochloride

Biological description

Kinase inhibitor, commonly used as a protein kinase A inhibitor (IC50 = 135 nM). Also inhibits other kinases, including MSK1 , S6K1 and ROCKII (IC50 values are 120, 80 and 270 nM, respectively).

Canonical smiles

C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCNCC=CC3=CC=C(C=C3)Br.Cl.Cl

Isomeric smiles

C1=CC2=C(C=CN=C2)C(=C1)S(=O)(=O)NCCNC/C=C/C3=CC=C(C=C3)Br.Cl.Cl

InChi

InChI=1S/C20H20BrN3O2S.2ClH/c21-18-8-6-16(7-9-18)3-2-11-22-13-14-24-27(25,26)20-5-1-4-17-15-23-12-10-19(17)20;;/h1-10,12,15,22,24H,11,13-14H2;2*1H/b3-2+;;

InChiKey

GELOGQJVGPIKAM-WTVBWJGASA-N

IUPAC Name

N-[2-[[(E)-3-(4-bromophenyl)prop-2-enyl]amino]ethyl]isoquinoline-5-sulfonamide;dihydrochloride

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

S6K1 AKT1 AKT2 and AKT3 are part of a group of serine/threonine kinases that play roles in cellular signaling. ROCK2 or Rho Kinase alpha is another serine/threonine kinase involved in regulating cytoskeletal dynamics. The cAMP Protein Kinase Catalytic subunit which includes PKA beta is important for many cellular processes through cAMP-dependent pathways. PRKACG is a catalytic subunit of PKA and has a molecular weight of about 40 kDa. These targets express widely in many tissues including muscle brain and liver where they have specific roles in diverse cellular activities.
Biological function summary

These kinases are essential in regulating proliferation survival and cell growth. S6K1 is critical in protein synthesis often linked with the mTOR complex. AKT isoforms (AKT1 AKT2 AKT3) control apoptosis and metabolism often in response to growth factors. ROCK2 influences smooth muscle contraction and cell motility. The cAMP Protein Kinase Catalytic subunit (including PKA) mediates responses to hormonal stimuli. They are often part of larger protein complexes impacting cellular reactions and maintaining homeostasis.

Pathways

These proteins are involved in important cellular signaling pathways like the PI3K/AKT/mTOR and RhoA/ROCK pathways. AKT1 AKT2 and AKT3 facilitate intracellular signaling impacting protein synthesis and glucose metabolism. S6K1 acts downstream of mTOR and works with these proteins to regulate cell growth and metabolism. ROCK2 functions in the regulation of actin cytoskeleton dynamics and interacts with other proteins like RhoA influencing cell shape and motility.

These targets relate to various pathological conditions like cancer and diabetes. Aberrant AKT signaling which includes AKT1 AKT2 and AKT3 is implicated in oncogenesis and tumor progression. The overactivity or dysregulation of mTOR/S6K1 signaling is pivotal in many cancers and metabolic disorders. ROCK2 dysregulation plays a role in hypertension and cardiac diseases influencing vascular tone and function. These kinases form potential therapeutic targets with inhibitors developed to modulate their activities in disease states.

Product protocols

Publications (8)

Recent publications for all applications. Explore the full list and refine your search

Brain sciences 14: PubMed38248228

2024

Activity of Protein Kinase A in the Frontal Cortex in Schizophrenia.

Applications

Unspecified application

Species

Unspecified reactive species

Smita Sahay,Nicholas Daniel Henkel,Christina Flora-Anabelle Vargas,Robert Erne McCullumsmith,Sinead Marie O'Donovan

The Journal of biological chemistry 299:102767 PubMed36470422

2022

Phosphorylation-dependent interactions of myosin-binding protein C and troponin coordinate the myofilament response to protein kinase A.

Applications

Unspecified application

Species

Unspecified reactive species

Ivanka R Sevrieva,Saraswathi Ponnam,Ziqian Yan,Malcolm Irving,Thomas Kampourakis,Yin-Biao Sun

Nature communications 13:674 PubMed35115535

2022

Gαi2-induced conductin/axin2 condensates inhibit Wnt/β-catenin signaling and suppress cancer growth.

Applications

Unspecified application

Species

Unspecified reactive species

Cezanne Miete,Gonzalo P Solis,Alexey Koval,Martina Brückner,Vladimir L Katanaev,Jürgen Behrens,Dominic B Bernkopf

Cell death & disease 12:134 PubMed33510128

2021

Extracellular vesicles-released parathyroid hormone-related protein from Lewis lung carcinoma induces lipolysis and adipose tissue browning in cancer cachexia.

Applications

Unspecified application

Species

Unspecified reactive species

Wenjun Hu,Hairong Xiong,Zeyuan Ru,Yan Zhao,Yali Zhou,Kairu Xie,Wen Xiao,Zhiyong Xiong,Cheng Wang,Changfei Yuan,Jian Shi,Quansheng Du,Xiaoping Zhang,Hongmei Yang

Journal of cellular and molecular medicine 24:8505-8517 PubMed32578931

2020

Cardiac β-adrenergic receptor activation mediates distinct and cell type-dependent changes in the expression and distribution of connexin 43.

Applications

Unspecified application

Species

Unspecified reactive species

Yi Zhang,Meng-Chen Hou,Jing-Jing Li,Ying Qi,Yu Zhang,Gang She,Yu-Jie Ren,Wei Wu,Zheng-Da Pang,Wenjun Xie,Xiu-Ling Deng,Xiao-Jun Du

Genes to cells : devoted to molecular & cellular m 25:197-214 PubMed31989743

2020

Prostaglandin E and its receptor EP2 trigger signaling that contributes to YAP-mediated cell competition.

Applications

Unspecified application

Species

Unspecified reactive species

Erika Ishihara,Yuya Nagaoka,Toshiaki Okuno,Satoshi Kofuji,Mari Ishigami-Yuasa,Hiroyuki Kagechika,Kenya Kamimura,Shuji Terai,Takehiko Yokomizo,Yukihiko Sugimoto,Yasuyuki Fujita,Akira Suzuki,Hiroshi Nishina

Applied physiology, nutrition, and metabolism = Physiologie appliquee, nutrition et metabolisme 45:227-239 PubMed31173696

2019

Resveratrol protects against nonalcoholic fatty liver disease by improving lipid metabolism and redox homeostasis via the PPARα pathway.

Applications

Unspecified application

Species

Unspecified reactive species

Yujie Huang,Hedong Lang,Ka Chen,Yong Zhang,Yanxiang Gao,Li Ran,Long Yi,Mantian Mi,Qianyong Zhang

Cell death & disease 9:305 PubMed29467389

2018

Long glucocorticoid-induced leucine zipper regulates human thyroid cancer cell proliferation.

Applications

Unspecified application

Species

Unspecified reactive species

Emira Ayroldi,Maria Grazia Petrillo,Maria Cristina Marchetti,Lorenza Cannarile,Simona Ronchetti,Erika Ricci,Luigi Cari,Nicola Avenia,Sonia Moretti,Efisio Puxeddu,Carlo Riccardi
View all publications

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