ChemicalBook > CAS DataBase List > SGC-GAK-1

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;SGC-GAK-1 ，S6710;SGC-GAK-1, 10 mM in DMSO;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: $108
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML2202
Product name: SGC-GAK-1
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $305.2
Updated: 2025/07/31

Tocris

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

Tocris

Product number: 6564
Product name: SGCGAK1
Purity: ≥99%(HPLC)
Packaging: 25
Price: $311
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] C. ASQUITH. SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)[J]. bioRxiv : the preprint server for biology, 2018, 163 1. DOI:10.1101/376772

SGC-GAK-1 Preparation Products And Raw materials

Raw materials

Preparation Products

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2226517-76-4, SGC-GAK-1Related Search:

AAK1 inhibitor 1 Ko 143 (E)-3-[[[3-[2-(7-CHLORO-2-QUINOLINYL)ETHENYL]PHENYL]-[[(3-DIMETHYLAMINO)-3-OXOPROPYL]THIO]METHYL]THIO]-PROPANOIC ACID, SODIUM SALT AAL-993 Cantharidin SGC2085 SGC707 SGC0946

SGC-GAK-1

GAK INHIBITOR 1

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

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

6-Bromo-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine

SGCGAK1,Inhibitor,SGC GAK 1,inhibit

S C- AK-1

SGC-GAK-1, 10 mM in DMSO

SGC-GAK-1 ，S6710

SGC-GAK-1 (GAK inhibitor 1)

2226517-76-4

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