2. PI3K/Akt/mTOR
  3. PDK-1
  4. PDK1-IN-RS2

PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1.

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PDK1-IN-RS2 Chemical Structure

PDK1-IN-RS2 Chemical Structure

CAS No. : 1643958-89-7

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Based on 1 publication(s) in Google Scholar

PDK1-IN-RS2 Related Antibodies

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Description

PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1[1].

IC50 & Target

Kd: 9 μM (PDK1)[1]
In Vitro

PDK1-IN-RS2 stimulates the catalytic activity of PDK1 toward a peptide substrate by sixfold. The sulfonyl group of PDK1-IN-RS2 interacts with Arg131 through a salt bridge, because the sulfonamide is likely ionized under the crystallization conditions[1].

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

PDK1-IN-RS2 Related Antibodies
Molecular Weight

380.89

Formula

C15H9ClN2O2S3
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=S(C1=CC2=CC=CC=C2S1)(NC3=NC4=CC=C(C=C4S3)Cl)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (328.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6254 mL 13.1271 mL 26.2543 mL
5 mM 0.5251 mL 2.6254 mL 5.2509 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
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. 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 2.6254 mL 13.1271 mL 26.2543 mL 65.6357 mL
5 mM 0.5251 mL 2.6254 mL 5.2509 mL 13.1271 mL
10 mM 0.2625 mL 1.3127 mL 2.6254 mL 6.5636 mL
15 mM 0.1750 mL 0.8751 mL 1.7503 mL 4.3757 mL
20 mM 0.1313 mL 0.6564 mL 1.3127 mL 3.2818 mL
25 mM 0.1050 mL 0.5251 mL 1.0502 mL 2.6254 mL
30 mM 0.0875 mL 0.4376 mL 0.8751 mL 2.1879 mL
40 mM 0.0656 mL 0.3282 mL 0.6564 mL 1.6409 mL
50 mM 0.0525 mL 0.2625 mL 0.5251 mL 1.3127 mL
60 mM 0.0438 mL 0.2188 mL 0.4376 mL 1.0939 mL
80 mM 0.0328 mL 0.1641 mL 0.3282 mL 0.8204 mL
100 mM 0.0263 mL 0.1313 mL 0.2625 mL 0.6564 mL
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PDK1-IN-RS2 Related Classifications

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.

Keywords:

PDK1-IN-RS21643958-89-7PDK-13-Phosphoinositide-dependent protein kinase 1S6K1catalyticsubstrateArg131PIFpocketLeu155sulfonyldiarylsulfonamideInhibitorinhibitorinhibit

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