1. PROTAC MAPK/ERK Pathway GPCR/G Protein PI3K/Akt/mTOR Membrane Transporter/Ion Channel
  2. Molecular Glues Ras PI3K GLUT
  3. DS02312223

DS02312223 (D223) is a molecular glue that promotes the binding of RAS to PI3Kα, with a Kd of 0.76 μM for p110α. DS02312223 increases the binding affinity between GTP-bound KRAS (KRAS-GMPPNP) and p110α by nearly three orders of magnitude (KD = 0.017 μM). DS02312223 stimulates the translocation of GLUT4 to the plasma membrane. DS02312223 promotes glucose uptake in the absence of insulin. DS02312223 can be used in diabetes research.

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DS02312223

DS02312223 Chemical Structure

CAS No. : 2253733-45-6

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Based on 1 publication(s) in Google Scholar

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Description

DS02312223 (D223) is a molecular glue that promotes the binding of RAS to PI3Kα, with a Kd of 0.76 μM for p110α. DS02312223 increases the binding affinity between GTP-bound KRAS (KRAS-GMPPNP) and p110α by nearly three orders of magnitude (KD = 0.017 μM). DS02312223 stimulates the translocation of GLUT4 to the plasma membrane. DS02312223 promotes glucose uptake in the absence of insulin. DS02312223 can be used in diabetes research[1].

IC50 & Target[1]

PI3Kα

 

GLUT4

 

In Vitro

DS02312223 (10-10000 nM) stimulates concentration-dependent GLUT4 translocation in differentiated L6-GLUT4 myc myotubes in the absence of insulin[1].
DS02312223 (1 μM; 5 min) enhances the interaction between PI3Kα and RRAS2 in serum-starved L6-GLUT4myc myotubes[1].
DS02312223 binds directly to p110α (KD = 0.76 μM) and increases the binding affinity between GTP-bound KRAS (KRAS-GMPPNP) and p110α by nearly three orders of magnitude (KD = 0.017 μM), but does not bind KRAS-GMPPNP or induce binding between KRAS-GDP and p110α[1].

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

Western Blot Analysis[1]

Cell Line: L6-GLUT4 myc myotubes
Concentration: 1 μM
Incubation Time: 5 min
Result: Increased the association of PI3Kα with RRAS2, whereas the inactive compound D484 had no effect.
Molecular Weight

581.66

Formula

C29H32FN5O5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(OC(NCCOCCOC1=C(C=CC=C1)C2=C3SC=CC3=C(N=N2)NC4=C(C=C(C=C4)CC(N)=O)F)=O)C

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 : 100 mg/mL (171.92 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 1.7192 mL 8.5961 mL 17.1922 mL
5 mM 0.3438 mL 1.7192 mL 3.4384 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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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 1.7192 mL 8.5961 mL 17.1922 mL 42.9804 mL
5 mM 0.3438 mL 1.7192 mL 3.4384 mL 8.5961 mL
10 mM 0.1719 mL 0.8596 mL 1.7192 mL 4.2980 mL
15 mM 0.1146 mL 0.5731 mL 1.1461 mL 2.8654 mL
20 mM 0.0860 mL 0.4298 mL 0.8596 mL 2.1490 mL
25 mM 0.0688 mL 0.3438 mL 0.6877 mL 1.7192 mL
30 mM 0.0573 mL 0.2865 mL 0.5731 mL 1.4327 mL
40 mM 0.0430 mL 0.2149 mL 0.4298 mL 1.0745 mL
50 mM 0.0344 mL 0.1719 mL 0.3438 mL 0.8596 mL
60 mM 0.0287 mL 0.1433 mL 0.2865 mL 0.7163 mL
80 mM 0.0215 mL 0.1075 mL 0.2149 mL 0.5373 mL
100 mM 0.0172 mL 0.0860 mL 0.1719 mL 0.4298 mL
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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:
DS02312223
Cat. No.:
HY-W1126235
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