2. Metabolic Enzyme/Protease Apoptosis
  3. Dipeptidyl Peptidase Apoptosis
  4. 1G244

1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.

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1G244 Chemical Structure

1G244 Chemical Structure

CAS No. : 847928-32-9

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Based on 3 publication(s) in Google Scholar

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Description

1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects[1][2].

IC50 & Target

DPP-4

 

In Vitro

1G244 (0-100 μM; 72 hours; Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells) treatment dose-dependently decreases viable cell number of five multiple myeloma cell lines[1].
1G244 (50 μM; 0-48 hours; MM.1 S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected[1].

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

1G244 Related Antibodies

Cell Viability Assay[1]

Cell Line: Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells
Concentration: 0 μM, 1 μM, 5 μM, 10 μM, 50 μM, or 100 μM
Incubation Time: 72 hours
Result: Dose-dependently decreased viable cell number of five multiple myeloma cell lines.

Western Blot Analysis[1]

Cell Line: MM.1 S cells
Concentration: 50 μM
Incubation Time: 0 hour, 3 hours, 6 hours, 12 hours, 24 hours, 48 hours
Result: Decreased caspase-3 and PARP protein.
In Vivo

1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1 S cells in murine xenograft model[1].

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

Animal Model: NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells[1]
Dosage: 30 mg/kg
Administration: Subcutaneous injection; once-a-week; for 3 weeks
Result: Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model.
Molecular Weight

504.57

Formula

C29H30F2N4O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1CC2=C(C=CC=C2)C1)[C@@H](N)CC(N3CCN(C(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (495.47 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 1.9819 mL 9.9094 mL 19.8189 mL
5 mM 0.3964 mL 1.9819 mL 3.9638 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.08 mg/mL (4.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
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).

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

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: 98.66%

COA (250 KB) LCMS (267 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 (sealed storage, away from moisture and light). 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 1.9819 mL 9.9094 mL 19.8189 mL 49.5471 mL
5 mM 0.3964 mL 1.9819 mL 3.9638 mL 9.9094 mL
10 mM 0.1982 mL 0.9909 mL 1.9819 mL 4.9547 mL
15 mM 0.1321 mL 0.6606 mL 1.3213 mL 3.3031 mL
20 mM 0.0991 mL 0.4955 mL 0.9909 mL 2.4774 mL
25 mM 0.0793 mL 0.3964 mL 0.7928 mL 1.9819 mL
30 mM 0.0661 mL 0.3303 mL 0.6606 mL 1.6516 mL
40 mM 0.0495 mL 0.2477 mL 0.4955 mL 1.2387 mL
50 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9909 mL
60 mM 0.0330 mL 0.1652 mL 0.3303 mL 0.8258 mL
80 mM 0.0248 mL 0.1239 mL 0.2477 mL 0.6193 mL
100 mM 0.0198 mL 0.0991 mL 0.1982 mL 0.4955 mL
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1G244 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:

1G244847928-32-9Dipeptidyl PeptidaseApoptosisDPPDipeptidylpeptidasesDPP8DPP9anti-myelomaapoptosiscelldeathcaspases-3PARPInhibitorinhibitorinhibit

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