1. MAPK/ERK Pathway
  2. p38 MAPK
  3. SB-747651A dihydrochloride

SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research.

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

SB-747651A dihydrochloride Chemical Structure

SB-747651A dihydrochloride Chemical Structure

CAS No. : 1781882-72-1

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Based on 1 publication(s) in Google Scholar

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Description

SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research[1].

IC50 & Target

IC50: 11 nM (MSK1)[1]

In Vitro

SB-747651A dihydrochloride (5 μM; neutrophils) affects CXCL2-induced intraluminal crawling of neutrophils in a Mac-1-dependent manner. SB-747651A dihydrochloride thwarts the intraluminal crawling of adherent neutrophils to optimal sites of emigration. SB-747651A dihydrochloride (5 μM; neutrophils) significantly increases transmigration time and detachment time. SB-747651A dihydrochloride affects mechanisms that regulate transendothelial migration of neutrophils in response to CXCL2 chemotactic gradient. SB-747651A dihydrochloride inhibits the migration speed of extravascular chemotaxing neutrophils but does not affect their directionality in response to CXCL2 chemotactic gradient[2].

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

In Vivo

SB747651A (3 mg/kg; intrascrotal injection) dihydrochloride results in increased neutrophil adhesion 3.5~4.5 hours following stimulation with CXCL2 as compared to the effect of CXCL2[3].
SB-747651A (3 mg/kg; i.p.) dihydrochloride affects neutrophil extravasation by increasing neutrophil emigration only at 3 and 4 hours in mouse peritonitis model of acute inflammation[3].

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

Animal Model: Male C57BL/6N mice (8~16 weeks)[3]
Dosage: 3 mg/kg
Administration: Intrascrotal injection
Result: Resulted in increased neutrophil adhesion 3.5~4.5 hours following stimulation with CXCL2 as compared to the effect of CXCL2.
Molecular Weight

415.32

Formula

C16H24Cl2N8O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NON=C1C(N2CC)=NC3=C2C(CNC4CCNCC4)=CN=C3.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (120.39 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4078 mL 12.0389 mL 24.0778 mL
5 mM 0.4816 mL 2.4078 mL 4.8156 mL
View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥99.0%

References

Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). 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
H2O 1 mM 2.4078 mL 12.0389 mL 24.0778 mL 60.1945 mL
5 mM 0.4816 mL 2.4078 mL 4.8156 mL 12.0389 mL
10 mM 0.2408 mL 1.2039 mL 2.4078 mL 6.0195 mL
15 mM 0.1605 mL 0.8026 mL 1.6052 mL 4.0130 mL
20 mM 0.1204 mL 0.6019 mL 1.2039 mL 3.0097 mL
25 mM 0.0963 mL 0.4816 mL 0.9631 mL 2.4078 mL
30 mM 0.0803 mL 0.4013 mL 0.8026 mL 2.0065 mL
40 mM 0.0602 mL 0.3010 mL 0.6019 mL 1.5049 mL
50 mM 0.0482 mL 0.2408 mL 0.4816 mL 1.2039 mL
60 mM 0.0401 mL 0.2006 mL 0.4013 mL 1.0032 mL
80 mM 0.0301 mL 0.1505 mL 0.3010 mL 0.7524 mL
100 mM 0.0241 mL 0.1204 mL 0.2408 mL 0.6019 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • 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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Product Name:
SB-747651A dihydrochloride
Cat. No.:
HY-110313
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