SGC-GAK-1

Product Name: SGC-GAK-1
CAS No.: 2226517-76-4
Chemical Name: SGC-GAK-1
Synonyms: S C- AK-1;SGC-GAK-1;GAK INHIBITOR 1;SGCGAK1,Inhibitor,SGC GAK 1,inhibit;6-Bromo-N-(3,4,5-trimethoxyphenyl)-4-quinolinamine;6-Bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine;4-Quinolinamine, 6-bromo-N-(3,4,5-trimethoxyphenyl)-
CBNumber: CB74742442
Molecular Formula: C18H17BrN2O3
Formula Weight: 389.24
MOL File: 2226517-76-4.mol

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SGC-GAK-1 Property

Boiling point:: 484.9±45.0 °C(Predicted)
Density: 1.436±0.06 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to 10 mg/ml)
form: powder
pka: 6.43±0.49(Predicted)
color: white to beige
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.

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Safety

HS Code: 2933499090

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML2202
Product name: SGC-GAK-1
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $105
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML2202
Product name: SGC-GAK-1
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $424
Updated: 2024/03/01

Tocris

Product number: 6564
Product name: SGCGAK1
Purity: ≥99%(HPLC)
Packaging: 25
Price: $311
Updated: 2021/12/16

Tocris

Product number: 6564
Product name: SGCGAK1
Purity: ≥99%(HPLC)
Packaging: 5
Price: $80
Updated: 2021/12/16

TRC

Product number: S282318
Product name: SGCGAK1
Packaging: 1mg
Price: $75
Updated: 2021/12/16

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SGC-GAK-1 Chemical Properties,Usage,Production

Description

SGC-GAK-1 (2226517-76-4) is a highly potent and selective inhibitor of cyclin G associated kinase (GAK), a member of the numb-associated kinase (NAK) family involved in membrane trafficking and sorting of proteins and is required for the maintenance of centrosome maturation and progression though mitosis. KD?= 1.9 nM with >50-fold selectivity against a panel of 400 kinases. It also displayed affinity for RIPK2 (KD?= 110 nM) and ADCK3 (KD?= 190 nM). SGC-GAK-1 displayed potent cellular activity in HEK293T cells (IC50?= 120 nM) and showed strong growth inhibition in the prostate cancer cell lines LNCaP (IC50?= 0.65 μM) and 22Rv1 (IC50?= 0.17 μM).

Uses

SGC GAK 1 is a high affinity cyclin G associated kinase (GAK) inhibitor (Kd = 1.9 nM). Exhibited >30-fold selectivity for GAK versus a panel of other kinases. Inhibits GAK in live cell assays (IC50 = 110 nM).

Biochem/physiol Actions

SGC-GAK-1 (CA93) is an ATP-competitive cyclin G-associated kinase (GAK) inhibitor (Ki = 3.1 nM by ATP site fluorescent tracer displacement assay; KD = 4.5 nM by ITC) that effectively inhibits Dengue viral entry and packaging in cultures (IC50 = 920 nM) without detectable cytotoxicity. SGC-GAK-1 exhibits much reduced affinity toward only 4 other kinases among a panel of ～400 (KD = 1.9 nM/GAK vs. 110 nM/RIPK2, 190 nM/ADCK3, 520 nM/NLK, 980 nM/AVCR1 by ligand competitive binding assay; IC50 = 110 nM/GAK vs. 360 nM/RIPK2 by cellular target engagement assay). SGC-GAK-1N (CA71) is a structure analog and the recommended negative control (GAK KD = 7.1 μM by ligand competitive binding assay; GAK & RIPK2 IC50 >50 μM by cellular target engagement assay). For characterization details of SGC-GAK-1, please visit the SGC-GAK-1 probe summary on the Structural Genomics Consortium (SGC) website.SGC-GAK-1N is the negative control for the active probe, SGC-GAK-1. SGC-GAK-1N is available from Sigma. To learn more about and purchase SGC-GAK-1N, click here.To learn about other SGC chemical probes, visit sigma.com/sgc

storage

Store at -20°C

References

1) Asquith?et al.?(2019),?SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK); J. Med. Chem.,?62?2830

SGC-GAK-1 Preparation Products And Raw materials

Raw materials

Preparation Products

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SGC-GAK-1 Suppliers

China 32 India 1 Japan 1 United Kingdom 1 United States 6 Global 41

Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: meilunui@163.com
Country: China
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Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4512
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Shanghaizehan biopharma technology co., Ltd.

Tel: 021-61350663 13052117465
Fax: 021-61350662
Email: sales@zehanbiopharma.com
Country: China
ProdList: 1009
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Tianjin Kailiqi Biotechnology Co., Ltd.

Tel: 15076683720
Fax: 022-23754520
Email: klq@cw-bio.com
Country: China
ProdList: 4602
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ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
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Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
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Shanghai SuperLan Chemcial Technique Centre

Tel: 021-2022843681 15618226720
Fax: +86-21-51601218
Email: lucy@atkchemical.com
Country: China
ProdList: 9204
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Amadis Chemical Company Limited

Tel: 571-89925085
Fax: 0086-571-89925065
Email: sales@amadischem.com
Country: China
ProdList: 131957
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Chuzhou KeMail Chemical Technology Co., Ltd

Tel: 0550-5196001 15000891977
Fax: 0550-5196001
Email: wj520wjxby@126.com
Country: China
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Taizhou Crene Biotechnology Co. Ltd.

Tel: +86-0576-88813233 +86-13396860566
Email: sales@pharm-intermediates.com
Country: China
ProdList: 1990
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2226517-76-4, SGC-GAK-1Related Search:

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SGC-GAK-1

GAK INHIBITOR 1

6-Bromo-N-(3,4,5-trimethoxyphenyl)-4-quinolinamine

4-Quinolinamine, 6-bromo-N-(3,4,5-trimethoxyphenyl)-

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SGCGAK1,Inhibitor,SGC GAK 1,inhibit

S C- AK-1

2226517-76-4

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