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
- Molecular Weight:
- 389.24
- MDL Number:
- MFCD31689258
- MOL File:
- 2226517-76-4.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| SGC-GAK-1 ≥98% (HPLC) | SML2202 | 5mg | $116 |
| SGC-GAK-1 ≥98% (HPLC) | SML2202 | 25mg | $467 |
| SGC-GAK-1 ≥98% | 33229 | 5mg | $41 |
| SGC-GAK-1 ≥98% | 33229 | 10mg | $72 |
| SGC-GAK-1 ≥98% | 33229 | 25mg | $140 |
| More product size | |||
| 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. |
| InChI | 1S/C18H17BrN2O3/c1-22-16-9-12(10-17(23-2)18(16)24-3)21-15-6-7-20-14-5-4-11(19)8-13(14)15/h4-10H,1-3H3,(H,20,21) |
| InChIKey | AUOSKLDNVNGKRR-UHFFFAOYSA-N |
| SMILES | BrC1=CC2=C(NC3=CC(OC)=C(OC)C(OC)=C3)C=CN=C2C=C1 |
| UNSPSC Code | 12352204 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| WGK Germany | WGK 3 |
|---|---|
| HS Code | 2933499090 |
| Storage Class | 11 - Combustible Solids |
SGC-GAK-1 price More Price(54)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML2202 | SGC-GAK-1 ≥98% (HPLC) | 2226517-76-4 | 5mg | $116 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML2202 | SGC-GAK-1 ≥98% (HPLC) | 2226517-76-4 | 25mg | $467 | 2026-04-30 | Buy |
| Cayman Chemical | 33229 | SGC-GAK-1 ≥98% | 2226517-76-4 | 5mg | $41 | 2026-04-30 | Buy |
| Cayman Chemical | 33229 | SGC-GAK-1 ≥98% | 2226517-76-4 | 10mg | $72 | 2026-04-30 | Buy |
| Cayman Chemical | 33229 | SGC-GAK-1 ≥98% | 2226517-76-4 | 25mg | $140 | 2026-04-30 | 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] 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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 | contact@trustwe.com | China | 5746 | 58 |
| Chemia Biotechnology（Shanghai） Co., Ltd | info@chemia-pharm.com | CHINA | 311 | 58 | |
| BOC Sciences | 16314854226; +8616314854226 | inquiry@bocsci.com | United States | 19853 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 | sales@sarms4muscle.com | China | 10457 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| HANGZHOU LEAP CHEM CO., LTD. | +86-571-87711850 +8619957148339 | market18@leapchem.com | China | 24597 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39037 | 58 |
| Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +86-15965530500 | nickzhang@hangyubiotech.com | China | 9942 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 |
