2. Membrane Transporter/Ion Channel PI3K/Akt/mTOR
  3. GLUT PI3K Akt
  4. D927

D927 (DS11252927) is an orally active glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM. D927 enhances the binding affinity of PI3Kα catalytic subunit p110α to canonical RAS proteins (KRAS4A, KRAS4B) and RRAS, RRAS2, MRAS. D927 activates the PI3Kα-AKT pathway (increasing phosphorylation of AKT, p70S6 kinase) without affecting the RAF-ERK1/2 pathway. D927 improves hyperglycemia in type 1 and type 2 diabetes mice model. D927 can be used for the study of glucose homeostasis disorders and diabetes.

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D927

D927 Chemical Structure

CAS No. : 2253733-37-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

D927 Related Antibodies

Top Publications Citing Use of Products

View All GLUT Isoform Specific Products:

View All Isoforms
GLUT1 GLUT2 GLUT3 GLUT4

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

D927 (DS11252927) is an orally active glucose transporter type 4 (GLUT4) translocation activator with an EC50 of 0.14 μM. D927 enhances the binding affinity of PI3Kα catalytic subunit p110α to canonical RAS proteins (KRAS4A, KRAS4B) and RRAS, RRAS2, MRAS. D927 activates the PI3Kα-AKT pathway (increasing phosphorylation of AKT, p70S6 kinase) without affecting the RAF-ERK1/2 pathway. D927 improves hyperglycemia in type 1 and type 2 diabetes mice model. D927 can be used for the study of glucose homeostasis disorders and diabetes[1][2].

IC50 & Target[1][2]

GLUT4

0.14 μM (EC50)

PI3Kα

 

In Vitro

D927 (Compound 26b) potently activates glucose transporter type 4 (GLUT4) translocation with an EC50 of 0.14 μM[1].
D927 (30-300 nM, 5 min) increases pAKT (Ser473) levels without affecting pMEK and pERK1/2 in various human cancer cell lines (PC3, RKO, SW1573, HCT15, SW620)[2].
D927 (10-10000 nM, 10 min) synergistically enhances insulin-induced AKT activation in L6 myotubes[2].
D927 (300 nM, 1-24 h) activates PI3Kα-AKT pathway by increasing phosphorylation of AKT (Ser473, Thr308) and p70S6 kinase (Thr389) in L6 myotubes without affecting RAF-ERK1/2 pathway[2].
D927 (1 μM, 1 h) promotes binding of KRAS (wild-type, G12D), MRAS, and RRAS2 to p110α in HEK293 cells[2].
D927 (600 nM, 5 min) induces pAKT (Ser473) accumulation mainly through RRAS2 in mouse embryo fibroblasts (MEFs)[2].

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

D927 Related Antibodies

Western Blot Analysis[2]

Cell Line: L6 myotubes
Concentration: 300 nM
Incubation Time: 1min, 10 min, 2h, 8h, 12h, 24 h
Result: Increased the phosphorylation of AKT (Ser473, Thr308) and p70S6 kinase (Thr389).
Had no substantial effect on the phosphorylation of ERK1/2 and MEK.

Western Blot Analysis[2]

Cell Line: Human cancer cell lines (RKO, SW1573, HCT15, SW620, PC3)
Concentration: 30, 300 nM
Incubation Time: 5 min
Result: Increased the phosphorylation of AKT (Ser473).

Western Blot Analysis[2]

Cell Line: L6 myotubes
Concentration: 10, 100, 1000, 10000 nM combined with 100 nM Insulin
Incubation Time: 10 min
Result: Increased the phosphorylation of AKT (Ser473).
Reduced the phosphorylation of AKT, ERK, and S6K.
In Vivo

D927 (Compound 26b) (3-30 mg/kg, p.o., single dose) shows a significant blood glucose lowering effect in the severe diabetic mice[1].
D927 (30 mg/kg, p.o., single dose 30 min before glucose infusion) shows glucose-lowering effects in Zucker fatty rats[2].
D927 (10 mg/kg, p.o., single dose 15 min before glucose loading) improves hyperglycemia in db/db mice (type 2 diabetes model) during oral glucose tolerance test[2].
D927 (0.01%-0.03%, p.o., 27 days) ameliorates hyperglycemia in STZ-B6 mice (type 1 diabetes model)[2].

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

Animal Model: Zucker fatty rats (overnight-fasted)[2]
Dosage: 30 mg/kg
Administration: p.o. for a single dose 30 min before glucose infusion
Result: Rapidly lowered blood glucose concentrations.
Increased glucose infusion rates and glucose turnover rates at steady state (90-120 min).
Significantly enhanced glucose uptake in soleus, gastrocnemius, and heart.
Decreased plasma insulin levels.
Animal Model: 10-week-old male db/db mice with high basal plasma glucose level (over 500 mg/mL) were used as the severe diabetic model, with 2 h-fasting before oral administration[1].
Dosage: 3, 10, 30 mg/kg
Administration: p.o. for a single dose
Result: Achieved significant blood glucose reduction with Emax values of 220 mg/dL, 393 mg/dL, and 435 mg/dL at doses of 3, 10, and 30 mg/kg, respectively.
Animal Model: 6-week-old db/db mice (type 2 diabetes model)[2]
Dosage: 10 mg/kg
Administration: p.o. for a single dose 15 min before glucose infusion
Result: Acutely improved hyperglycemia in oral glucose tolerance test, with reduced blood glucose AUC (0-120 min).
Did not affect insulin secretion during acute treatment.
After 24 days of chronic administration, significantly reduced glycated hemoglobin, with effects comparable to insulin.
No change in food intake.
Animal Model: STZ-B6 mice (type 1 diabetes model, insulin-deficient)[2]
Dosage: 0.01%, 0.03%
Administration: p.o. for 27 days
Result: Reduced glycated hemoglobin, with effects comparable to 0.1 U/day insulin.
No change in food intake.
Increased body and tissue weight.
Molecular Weight

452.50

Formula

C23H21FN4O3S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

COCCOC1=CC=CC=C1C2=C(SC=C3)C3=C(NC4=CC=C(CC(N)=O)C=C4F)N=N2
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 (220.99 mM; ultrasonic and warming and heat to 60°C; 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 2.2099 mL 11.0497 mL 22.0994 mL
5 mM 0.4420 mL 2.2099 mL 4.4199 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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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

Concentration (start)

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In Vivo:

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

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: ≥ 2.5 mg/mL (5.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.46%

SDS (251 KB)

COA (257 KB) HNMR (303 KB) LCMS (102 KB)

Handling Instructions (2659 KB)
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 2.2099 mL 11.0497 mL 22.0994 mL 55.2486 mL
5 mM 0.4420 mL 2.2099 mL 4.4199 mL 11.0497 mL
10 mM 0.2210 mL 1.1050 mL 2.2099 mL 5.5249 mL
15 mM 0.1473 mL 0.7366 mL 1.4733 mL 3.6832 mL
20 mM 0.1105 mL 0.5525 mL 1.1050 mL 2.7624 mL
25 mM 0.0884 mL 0.4420 mL 0.8840 mL 2.2099 mL
30 mM 0.0737 mL 0.3683 mL 0.7366 mL 1.8416 mL
40 mM 0.0552 mL 0.2762 mL 0.5525 mL 1.3812 mL
50 mM 0.0442 mL 0.2210 mL 0.4420 mL 1.1050 mL
60 mM 0.0368 mL 0.1842 mL 0.3683 mL 0.9208 mL
80 mM 0.0276 mL 0.1381 mL 0.2762 mL 0.6906 mL
100 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5525 mL
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D927 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:

D9272253733-37-6DS11252927D 927D-927DS 11252927DS-11252927GLUTPI3KAktGlucose transporter Phosphoinositide 3-kinasePKBProtein kinase Bdiabeticdb/dbmicehypoglycemicglucose homeostasis disordersGLUT4PI3Kα-AKTInhibitorinhibitorinhibit

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