1. Cell Cycle/DNA Damage
  2. Cyclin G-associated Kinase (GAK)
  3. SGC-GAK-1

SGC-GAK-1 

Cat. No.: HY-122186 Purity: 99.77%
COA Handling Instructions

SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a Ki of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK.

For research use only. We do not sell to patients.

SGC-GAK-1 Chemical Structure

SGC-GAK-1 Chemical Structure

CAS No. : 2226517-76-4

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Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 99 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 300 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
100 mg USD 760 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SGC-GAK-1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a Ki 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 Kis 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 KDs 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 IC50s of 0.05±0.15 µM and 0.17±0.65 µM, respectively.
Molecular Weight

389.24

Formula

C18H17BrN2O3

CAS No.
SMILES

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

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
In Vitro: 

DMSO : 41.67 mg/mL (107.05 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.34 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (5.34 mM); Clear solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.34 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.77%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SGC-GAK-1
Cat. No.:
HY-122186
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