SGC-GAK-1
- CAS No.
- 2226517-76-4
- Chemical Name:
- SGC-GAK-1
- Synonyms
- 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
- Molecular Weight:
- 389.24
- MDL Number:
- MFCD31689258
- MOL File:
- 2226517-76-4.mol
| 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) |
| pka | 6.43±0.49(Predicted) |
| form | powder |
| 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. |
SGC-GAK-1 price More Price(16)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML2202 | SGC-GAK-1 ≥98% (HPLC) | 2226517-76-4 | 5mg | $105 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML2202 | SGC-GAK-1 ≥98% (HPLC) | 2226517-76-4 | 25mg | $424 | 2024-03-01 | Buy |
| Tocris | 6564 | SGCGAK1 ≥99%(HPLC) | 2226517-76-4 | 25 | $311 | 2021-12-16 | Buy |
| Tocris | 6564 | SGCGAK1 ≥99%(HPLC) | 2226517-76-4 | 5 | $80 | 2021-12-16 | Buy |
| TRC | S282318 | SGCGAK1 | 2226517-76-4 | 1mg | $75 | 2021-12-16 | Buy |
SGC-GAK-1 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 +8618813727289 | contact@trustwe.com | China | 5738 | 58 |
| Chemia Biotechnology（Shanghai） Co., Ltd | +8613816753574 | info@chemia-pharm.com | CHINA | 311 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |