SGC-GAK-1 | CAS# 2226517-76-4 | GAK Probe

MedKoo Cat#: 564186 | Name: SGC-GAK-1

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SGC-GAK-1 is a potent and selective GAK kinase probe which targets the ATP-binding site.

Chemical Structure

SGC-GAK-1

CAS#2226517-76-4

Theoretical Analysis

MedKoo Cat#: 564186

Name: SGC-GAK-1

CAS#: 2226517-76-4

Chemical Formula: C18H17BrN2O3

Exact Mass: 388.0423

Molecular Weight: 389.25

Elemental Analysis: C, 55.54; H, 4.40; Br, 20.53; N, 7.20; O, 12.33

Price and Availability

Size	Price	Availability
10mg	USD 250.00	2 Weeks
25mg	USD 450.00	2 Weeks
50mg	USD 700.00	2 Weeks
200mg	USD 1,650.00	2 Weeks
500mg	USD 2,250.00	2 Weeks
1g	USD 3,250.00	2 Weeks
2g	USD 5,850.00	2 Weeks

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Synonym

SGCGAK1; SGC GAK 1; SGC-GAK-1; SGCGAK-1; SGC-GAK1

IUPAC/Chemical Name

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

InChi Key

AUOSKLDNVNGKRR-UHFFFAOYSA-N

InChi Code

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)

SMILES Code

COC1=C(OC)C(OC)=CC(NC2=CC=NC3=CC=C(Br)C=C23)=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO and ethanol

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.03.00

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

SGC-GAK-1 is a high affinity GAK inhibitor (Kd = 1.9 nM) and exhibits >30-fold selectivity for GAK over a panel of other kinases. SGC-GAK-1 inhibits GAK in live cell assays (IC50 = 110 nM).

In vitro activity:

GAK may be physiologically involved in normal neuronal development, and decreased GAK function and the resulting impaired neurite outgrowth and synaptogenesis may be related to neurodevelopmental disorders. SGC-GAK-1 treatment of cultured neurons reduced neurite length and decreased synapse number and phosphorylation of neurofilament 200-kDa subunits relative to the control. I Reference: Mol Brain. 2022 Jul 26;15(1):68. https://pubmed.ncbi.nlm.nih.gov/35883152/

In vivo activity:

To be determined

	Solvent	mg/mL	mM
Solubility
	DMSO	38.9	100.00
	Ethanol	19.5	50.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 389.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Egawa J, Arta RK, Lemmon VP, Muños-Barrero M, Shi Y, Igarashi M, Someya T. The cyclin G-associated kinase (GAK) inhibitor SGC-GAK-1 inhibits neurite outgrowth and synapse formation. Mol Brain. 2022 Jul 26;15(1):68. doi: 10.1186/s13041-022-00951-6. PMID: 35883152; PMCID: PMC9327206.

In vitro protocol:

In vivo protocol: