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AB120341

H89 dihydrochloride, Kinase inhibitor

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(6 제품이 사용된 논문 )

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).

대체 명칭 보기

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

2 이미지
Functional Studies - H89 dihydrochloride, Kinase inhibitor (AB120341)
  • FuncS

PubMed

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.

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/

Chemical Structure - H89 dihydrochloride, Kinase inhibitor (AB120341)
  • Chemical Structure

Lab

Chemical Structure - H89 dihydrochloride, Kinase inhibitor (AB120341)

2D chemical structure image of ab120341, H89 dihydrochloride, Kinase inhibitor

주요 정보

CAS 번호

130964-39-5

Purity

>98%

제형

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

생화학적 명칭

H-89 Dihydrochloride

생물학적 정보

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

특성 및 보관 정보

배송 시 보관 조건
Ambient - Can Ship with Ice
적절한 단기 보관 조건
-20°C
적절한 장기 보관 조건
-20°C
보관 정보
Store under desiccating conditions|The product can be stored for up to 12 months
취급 방법

Need more advice on solubility, usage and handling? Please visit our our product support page for more details.

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Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

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Refer to SDS for further information.

추가 정보

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

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.

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.

제품 프로토콜

제품이 사용된 논문 (6)

Recent publications for all applications. Explore the 전체 목록 and refine your search

Scientific reports 12:21158 PubMed36477209

2022

Npp1 prevents external tooth root resorption by regulation of cervical cementum integrity.

Applications

Unspecified application

Species

Unspecified reactive species

Hwajung Choi,Liu Yang,Yudong Liu,Ju-Kyung Jeong,Eui-Sic Cho

Cell reports 35:109076 PubMed33951438

2021

Aging-dependent mitochondrial dysfunction mediated by ceramide signaling inhibits antitumor T cell response.

Applications

Unspecified application

Species

Unspecified reactive species

Silvia 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 Ogretmen

Cell reports 34:108899 PubMed33761345

2021

Activity- and sleep-dependent regulation of tonic inhibition by Shisa7.

Applications

Unspecified application

Species

Unspecified reactive species

Kunwei Wu,Wenyan Han,Qingjun Tian,Yan Li,Wei Lu

Scientific reports 6:26608 PubMed27197559

2016

Cyp2aa9 regulates haematopoietic stem cell development in zebrafish.

Applications

Unspecified application

Species

Unspecified reactive species

Jingying Chen,Jianbo He,Li Li,Deqin Yang,Lingfei Luo

PloS one 10:e0128678 PubMed26030901

2015

UVB 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 application

Species

Unspecified reactive species

Hideki Tagashira,Aki Miyamoto,Sei-Ichi Kitamura,Masahito Tsubata,Kazuya Yamaguchi,Kinya Takagaki,Genji Imokawa

The Journal of neuroscience : the official journal of the Society for Neuroscience 33:5006-16 PubMed23486971

2013

The slow afterhyperpolarization: a target of β1-adrenergic signaling in hippocampus-dependent memory retrieval.

Applications

Unspecified application

Species

Unspecified reactive species

Lei Zhang,Ming Ouyang,C Robin Ganellin,Steven A Thomas
제품이 사용된 논문 모두 보기

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