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).
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- Scientific reports 12:211582022Npp1 prevents external tooth root resorption by regulation of cervical cementum integrity.Applications:Unspecified applicationReactive species:Unspecified reactive speciesHwajung Choi,Liu Yang,Yudong Liu,Ju-Kyung Jeong,Eui-Sic ChoPubMed 36477209
- Cell reports 35:1090762021Aging-dependent mitochondrial dysfunction mediated by ceramide signaling inhibits antitumor T cell response.Applications:Unspecified applicationReactive species:Unspecified reactive speciesSilvia Vaena,Paramita Chakraborty,Han Gyul Lee,Alhaji H Janneh,Mohamed Faisal Kassir,Gyda Beeson,Zachariah Hedley,Ahmet Yalcinkaya,M Hanief Sofi,Hong Li,Monica L Husby,Robert V Stahelin,Xue-Zhong Yu,Shikhar Mehrotra,Besim OgretmenPubMed 33951438
- Cell reports 34:1088992021Activity- and sleep-dependent regulation of tonic inhibition by Shisa7.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKunwei Wu,Wenyan Han,Qingjun Tian,Yan Li,Wei LuPubMed 33761345
- Scientific reports 6:266082016Cyp2aa9 regulates haematopoietic stem cell development in zebrafish.Applications:Unspecified applicationReactive species:Unspecified reactive speciesJingying Chen et. al.PubMed 27197559
- PloS one 10:e01286782015UVB Stimulates the Expression of Endothelin B Receptor in Human Melanocytes via a Sequential Activation of the p38/MSK1/CREB/MITF Pathway Which Can Be Interrupted by a French Maritime Pine Bark Extract through a Direct Inactivation of MSK1.Applications:Unspecified applicationReactive species:Unspecified reactive speciesHideki Tagashira et. al.PubMed 26030901
- The Journal of neuroscience : the official journal of the Society for Neuroscience 33:5006-162013The slow afterhyperpolarization: a target of β1-adrenergic signaling in hippocampus-dependent memory retrieval.Applications:Unspecified applicationReactive species:Unspecified reactive speciesLei Zhang,Ming Ouyang,C Robin Ganellin,Steven A ThomasPubMed 23486971
Key facts
- CAS number
- 130964-39-5
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 519.3 Da
- Molecular formula
- C20H22BrCl2N3O2S
- PubChem identifier
- 5702541
- Nature
- Synthetic
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
Recommended products
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).
Key facts
- CAS number
- 130964-39-5
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 519.3 Da
- Molecular formula
- C20H22BrCl2N3O2S
- PubChem identifier
- 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
Storage
- 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 info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
AKT3 also known as Protein Kinase B gamma is a serine/threonine kinase that plays an important role in cell survival and metabolism. Along with AKT2 a closely related isoform AKT3 shares structural similarities but differs in tissue distribution and specific functions. AKT3 has a molecular weight of approximately 56 kDa. It is expressed in brain heart and testis tissues. Its catalytic activity is regulated by phosphorylation at two key residues contributing to its activation state.
- Biological function summary
AKT3 and AKT2 influence processes like glucose uptake cell proliferation and suppression of apoptosis. These proteins do not form a stable complex but interact with other proteins as part of their activation and signaling processes. The cAMP Protein Kinase Catalytic subunit often called PKA C or PKAc is involved in similar pathways regulating numerous cellular processes through phosphorylation events. ROCK2 or Rho-associated coiled-coil containing protein kinase 2 acts in cytoskeletal dynamics influencing cell shape and movement.
- Pathways
AKT3 participates in the PI3K/AKT signaling pathway important for transmitting extracellular signals into the cell influencing growth and survival. In this pathway AKT3 and AKT2 interact with proteins like mTOR and GSK-3 which help regulate cell cycle progression and metabolism. ROCK2 is mainly involved in the RhoA/ROCK pathway modulating actin cytoskeleton organization and affecting processes such as contraction cell migration and proliferation.
- Associated diseases and disorders
AKT3 and AKT2 have been linked to cancer and insulin resistance. Mutations or aberrant activation can lead to excessive cell growth and survival contributing to tumorigenesis. Similarly dysregulation of AKT3 and AKT2 signaling can cause insulin resistance affecting glucose homeostasis. ROCK2 is connected to cardiovascular diseases influencing blood vessel tone and heart function. These proteins by being integral to these disease pathways present potential therapeutic targets and the use of kinase inhibitors like those targeting AKT and ROCK pathways can modulate their activity in disease contexts.
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2 product images
Chemical Structure - H89 dihydrochloride, Kinase inhibitor (ab120341)
2D chemical structure image of ab120341, H89 dihydrochloride, Kinase inhibitor
Image from Tagashira, Hideki et al., PLOS One., 10(6):e0128678. Fig 8.; doi: 10.1371/journal.pone.0128678. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/Functional Studies - H89 dihydrochloride, Kinase inhibitor (ab120341)
Normal human melanocytes (NHMs) were treated with ab120341 at the indicated concentrations to test if the inhibition of MSK1 activation results in the down-regulated MITF and EDNRB expression in UVB-exposed NHMs. ab120341 was added immediately after UVB irradiation and cells were cultured for 6h (for MITF, A) or 24 h (for EDNRB, B). Total mRNAs were purified and Real-time RT-PCR was carried out with MITF or EDNRB primer and β-actin primer as the internal control. Error bars represent S.D. from triplicate experiments. *P<0.05 and **P<0.01 against NHMs UVB-irradiated in the absence of H89, respectively.
Tagashira, Hideki et al., PLOS One., 10(6):e0128678. Fig 8.; doi: 10.1371/journal.pone.0128678.
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