- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Bioactive Molecules
- Anti-infection
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
- Methylation
- Cytoskeletal Signaling
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 2226517-76-4] SGC-GAK-1
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-122186 |
| Brand: | MCE |
| CAS: | 2226517-76-4 |
Overview
| MDL | MFCD31689258 |
|---|---|
| Molecular Weight | 389.24 |
| Molecular Formula | C18H17BrN2O3 |
| SMILES | COC1=C(C(OC)=CC(NC2=CC=NC3=CC=C(C=C23)Br)=C1)OC |
1 Publications Citing Use of MCE
Summary
SGC-GAK-1 is a potent, selective cyclin G-associated kinase ( GAK ) inhibitor with a K i of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK [1] .
IC50 & Target
Ki: 3.1 nM (GAK) [1]
In Vitro
SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), adaptor protein 2-associated kinase (AAK1), serine/threonine kinase 16 (STK16) with K
i
s of 3.1 nM, 53 µM, 51 µM, respectively
[1]
.
SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), receptor-interacting protein kinase 2 (RIPK2), AarF domain containing kinase 3 (ADCK3), and nemo-like kinase (NLK) with K
D
s of 1.9 nM, 110 nM, 190 nM, and 520 nM, respectively
[1]
.
SGCGAK-1 (0.1, 1, and 10 µM, 48 hours or 72 hours) shows strong growth inhibition in LNCaP, VCaP, and 22Rv1 cells at 10 µM, but minimal effect in PC3 and DU145 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | Prostate cancer cells (22Rv1, LNCaP, VCaP, PC3, DU145) |
| Concentration: | 0.1, 1, and 10 µM |
| Incubation Time: | 48 hours or 72 hours |
| Result: | Showed potent antiproliferative activity in LNCaP and 22Rv1 cells with IC 50 s of 0.05±0.15 µM and 0.17±0.65 µM, respectively. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 41.67 mg/mL ( 107.05 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5691 mL | 12.8455 mL | 25.6911 mL |
| 5 mM | 0.5138 mL | 2.5691 mL | 5.1382 mL |
| 10 mM | 0.2569 mL | 1.2846 mL | 2.5691 mL |
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.