2. Protein Tyrosine Kinase/RTK
    Autophagy
    Stem Cell/Wnt
    PI3K/Akt/mTOR
    JAK/STAT Signaling
    Epigenetics
    Cell Cycle/DNA Damage
  3. Syk
    Src
    LRRK2
    GSK-3
    JAK
    VEGFR
    Aurora Kinase
  4. GSK2646264

GSK2646264 

Cat. No.: HY-112809 Purity: 98.39%
COA Handling Instructions

GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin.

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

GSK2646264 Chemical Structure

GSK2646264 Chemical Structure

CAS No. : 1398695-47-0

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5 mg USD 800 In-stock
10 mg USD 1280 In-stock
25 mg USD 2550 In-stock
50 mg USD 4050 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

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JAK1 JAK2 JAK3 Tyk2 JAK

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All Aurora Kinase Isoform Specific Products:

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Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin[1].

IC50 & Target

SYK

7.1 (pIC50)

LCK

5.4 (pIC50)

LRRK2

5.4 (pIC50)

GSK3β

5.3 (pIC50)

JAK2

5 (pIC50)

VEGFR2

4.5 (pIC50)

Aurora B

<4.6 (pIC50)

Aurora A

<4.3 (pIC50)

In Vitro

GSK2646264 (0.01-10 μM; 1 h) significantly inhibits anti‐IgE (but not C5a)‐induced histamine release from skin mast cells in a concentration‐dependent manner. The IC50 is 0.7 μM and the IC90 is 6.8 μM[2].
GSK2646264 cream (0.5, 1, and 3% [wt/wt]; 1 cm2; 4 and 24 h) inhibits anti‐IgE‐induced histamine release from mast cells in ex vivo human skin[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

374.48

Appearance

Solid

Formula

C24H26N2O2
CAS No.
SMILES

CC1=CC(COC2=C(C3=CC=C4CCNCCC4=C3)C(OC)=CC=C2)=NC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (133.52 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6704 mL 13.3518 mL 26.7037 mL
5 mM 0.5341 mL 2.6704 mL 5.3407 mL
10 mM 0.2670 mL 1.3352 mL 2.6704 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: ≥ 1.25 mg/mL (3.34 mM); Clear solution

  • 2.

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

    Solubility: ≥ 1.25 mg/mL (3.34 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1.25 mg/mL (3.34 mM); Clear solution

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

Purity: 98.39%

COA (256 KB) HNMR (222 KB) RP-HPLC (254 KB)

Handling Instructions (2659 KB)
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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Keywords:

GSK26462641398695-47-0GSK 2646264GSK-2646264SykSrcLRRK2GSK-3JAKVEGFRAurora KinaseSpleen tyrosine kinaseLeucine-rich repeat kinase 2Glycogen synthase kinase-3Glycogen synthase kinase 3Janus kinaseVascular endothelial growth factor receptorinflammatory skinskin penetrationInhibitorinhibitorinhibit

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