Cat. No.: HY-132296

GSK215

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC₅₀ of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.
(Pink: FAK ligand (HY-13917); Blue: VHL ligand (HY-112078); Black: linker).

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Pureté: 99.26%
CAS No.: 2743427-26-9
Formule: C₅₀H₅₉F₃N₁₀O₆S
Masse moléculaire:985.13

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GSK215 Chemical Structure

CAS No.: 2743427-26-9

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
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Activité biologique

Description

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC₅₀ of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect^[1]. (Pink: FAK ligand (HY-13917); Blue: VHL ligand (HY-112078); Black: linker).

IC₅₀ & Target

PROTAC; pDC₅₀: 8.4 (FAK)^[1]

Voir tous les produits spécifiques à Isoform PROTACs :

In Vitro

GSK215 (0.1-1000 nM; 2 h) effectively increases the FAK degradation by >90% and determines a DC₅₀ of 1.3 nM in A549 cells^[1].
GSK215 induced degradation is proteasome and ubiquitin dependent^[1].
GSK215 (above 100 nM, 6h) reduces primarily kinases CDK7, RPS6KA3, MET and GAK^[1].
GSK215 (100 nM, 48 h) inhibits migration, invasion and collagen deposition in A549 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

A549 cells
Concentration:

0.1-1000 nM
Incubation Time:

2 h
Result:

Increased the FAK degradation.

Cell Migration Assay ^[1]

Cell Line:

A549 cells
Concentration:

100 nM
Incubation Time:

48 h
Result:

Inhibited cell migration.

Cell Invasion Assay^[1]

Cell Line:

A549 cells
Concentration:

100 nM
Incubation Time:

48 h
Result:

Inhibited cell invasion.

In Vivo

GSK215 (8 mg/kg; i.h.; once) degrades FAK, and shows the C_max and t_max values of 526 ng/mL and 0.33 hours, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male CD1 mice (P878/881A), 7-9 weeks^[1]
Dosage:

8 mg/kg
Administration:

Single subcutaneous injection
Result:

Caused a rapid and profound degradation of FAK in liver over time, with a maximal degradation of ~85% being achieved within 18 h. Endogenous FAK was found to still be reduced by ~60% at 96 h post-dose.The C_max and t_max were 526 ng/mL and 0.33 hours, respectively.

Chemical Information

CAS No. 2743427-26-9
Appearance Solid
Masse moléculaire 985.13
Formule C₅₀H₅₉F₃N₁₀O₆S
Color Off-white to light yellow
SMILES

O=C([C@H]1N(C([C@@H](NC(CN2CCN(C3=CC=C(NC4=NC=C(C(F)(F)F)C(NC5=CC=CC=C5C(NC)=O)=C4)C(OC)=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Sci Adv

Inhibition of focal adhesion kinase impairs tumor formation and preserves hearing in a murine model of NF2-related schwannomatosis. [Abstract]

2026 Jan 30;12(5):eady8382. PMID: 41616055
Cell Signal

The role of FAK signaling in early placental development and trophoblast lineage specification in human pregnancy. [Abstract]

2025 Jun 17:111946. PMID: 40553964

Solvant et solubilité

In Vitro:

DMSO : 250 mg/mL (253.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0151 mL

5.0755 mL

10.1509 mL

5 mM

0.2030 mL

1.0151 mL

2.0302 mL

10 mM

0.1015 mL

0.5075 mL

1.0151 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.08 mg/mL (2.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (2.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (393 KB)
- English - EN (393 KB)
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- Deutsch - DE (393 KB)
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- Español - ES (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Law RP, Nunes J, Chung CW, et al. Discovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs [published online ahead of print, 2021 Aug 20]. Angew Chem Int Ed Engl. 2021;10.1002/anie.202109237. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0151 mL	5.0755 mL	10.1509 mL	25.3774 mL
	5 mM	0.2030 mL	1.0151 mL	2.0302 mL	5.0755 mL
	10 mM	0.1015 mL	0.5075 mL	1.0151 mL	2.5377 mL
	15 mM	0.0677 mL	0.3384 mL	0.6767 mL	1.6918 mL
	20 mM	0.0508 mL	0.2538 mL	0.5075 mL	1.2689 mL
	25 mM	0.0406 mL	0.2030 mL	0.4060 mL	1.0151 mL
	30 mM	0.0338 mL	0.1692 mL	0.3384 mL	0.8459 mL
	40 mM	0.0254 mL	0.1269 mL	0.2538 mL	0.6344 mL
	50 mM	0.0203 mL	0.1015 mL	0.2030 mL	0.5075 mL
	60 mM	0.0169 mL	0.0846 mL	0.1692 mL	0.4230 mL
	80 mM	0.0127 mL	0.0634 mL	0.1269 mL	0.3172 mL
	100 mM	0.0102 mL	0.0508 mL	0.1015 mL	0.2538 mL

Keywords

GSK215

2 Cited Publications

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GSK215

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK215

Voir tous les produits spécifiques à Isoform PROTACs

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GSK215

Heterocyclic Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK215

Voir tous les produits spécifiques à Isoform PROTACs

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GSK215 Related Classifications

HY-132296 Related Classifications