Cat. No.: HY-163828

PPA24

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PPA24 is a PP2A activator with a K_D of 8.465 μM for PP2ACα. PPA24 induces cancer cell death via apoptosis. PP2ACα induces ROS generation and decreases the level of c-Myc expression. PPA24 can be used to study colorectal cancer (CRC), Folinic acid (HY-17556), 5-Fluorouracil (HY-90006), and Oxaliplatin (HY-17371) (FOLFOX)-resistant CRC, and melanoma cancer.

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Pureté: 98.09%
CAS No.: 3035032-77-7
Formule: C₂₂H₂₇BrClN₅S
Masse moléculaire:508.91

Stockage:

4°C, sealed storage, away from moisture

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

PPA24 Chemical Structure

CAS No.: 3035032-77-7

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

PP2A

GSK-3α

GSK-3β

Voir tous les produits spécifiques à Isoform GSK-3 :

Voir tous les produits spécifiques à Isoform ERK :

In Vitro

PPA24 (0.5-50 μM, 48 h) shows cytotoxicity against HCT116, HT29, DLD1, SW480, FOLFOX HCT116 and FOLFOX HT29, with IC₅₀s of 3.95, 6.75, 3.45, 3.64, 2.63 and 3.04 μM, respectively, shows weak cytotoxicity against HaCaT, with IC₅₀ of 10.04 μM^[1].
PPA24 (2.5-10 μM, 24 h) induces apoptosis in HCT116, HT29, FOLFOX HCT116, FOLFOX HT29 cells^[1].
PPA24 (2.5-5 μM, 6-12 h) stimulates ROS generation in HCT116 cells^[1].
PPA24 (2.5-5 μM, 24 h) decreases the level of c-Myc expression in HCT116, FOLFOX HCT116 cells^[1].
PPA24 (0.1-10 μM, 48 h) shows a synergistic effect and Gemcitabine (HY-17026) or Cisplatin (HY-17394) with HCT116 cells^[1].
PPA24 shows cytotoxicity against SK-MEL-2, SK-MEL-28, A375, Mel1241, and 451Lu cells with IC₅₀s in the range of 5.99-14.45 μM^[3].

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

Apoptosis Analysis^[1]

Cell Line:

HCT116, HT29, FOLFOX HCT116, FOLFOX HT29
Concentration:

2.5 μM, 5 μM, 10 μM
Incubation Time:

24 h
Result:

Induced apoptosis.

Western Blot Analysis^[1]

Cell Line:

HCT116, FOLFOX HCT116
Concentration:

2.5 μM, 5 μM
Incubation Time:

24 h
Result:

Decreased the level of c-Myc expression, did not increase the level of degradation of c-Myc.
Reduced the protein expression level of GSK-3α/β but did not change p-GSK-3α/β (S21/9).

In Vivo

PPA24 (nanoformulation (Nano-PPA24)) (6 mg/kg, i.v., three times per week, 23 days) inhibits tumor growth with no significant changes in body weight in HCT116 xenografts nude mice model^[1].

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

Animal Model:

HCT116 (1.5 × 10⁶) xenografts nude mice model^[1]
Dosage:

6 mg/kg, nanoformulation (Nano-PPA24)
Administration:

i.v., three times per week, 23 days
Result:

Inhibited tumor growth with no significant changes in body weight.

Chemical Information

CAS No. 3035032-77-7
Appearance Solid
Masse moléculaire 508.91
Formule C₂₂H₂₇BrClN₅S
Color White to off-white
SMILES

ClC1=CC=C2C(N(C3=CC=CC=C3S2)CCCC[N+]4(C[N@@](C5)C6)C[N@@]6C[N@@]5C4)=C1.[Br-]
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

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

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (196.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9650 mL

9.8249 mL

19.6498 mL

5 mM

0.3930 mL

1.9650 mL

3.9300 mL

10 mM

0.1965 mL

0.9825 mL

1.9650 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 (4.91 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (4.91 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Español - ES (252 KB)
- Swedish - SV (252 KB)
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- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Johnson H, et al. Identification of a Novel Protein Phosphatase 2A Activator, PPA24, as a Potential Therapeutic for FOLFOX-Resistant Colorectal Cancer. J Med Chem. 2024 Oct 24;67(20):18070-18089. [Content Brief]

[2]. Hannah Johnson, et al.Sharma; Abstract 1655: Discovery of a novel PP2A activator as a potential therapeutic for FOLFOX resistant colon cancer. Cancer Res 1 April 2023; 83 (7_Supplement): 1655.

[3]. Hannah Johnson, et al. Abstract 7273: Small molecule activation of PP2A in the treatment of melanoma. Cancer Res 15 March 2024; 84 (6_Supplement): 7273.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9650 mL	9.8249 mL	19.6498 mL	49.1246 mL
	5 mM	0.3930 mL	1.9650 mL	3.9300 mL	9.8249 mL
	10 mM	0.1965 mL	0.9825 mL	1.9650 mL	4.9125 mL
	15 mM	0.1310 mL	0.6550 mL	1.3100 mL	3.2750 mL
	20 mM	0.0982 mL	0.4912 mL	0.9825 mL	2.4562 mL
	25 mM	0.0786 mL	0.3930 mL	0.7860 mL	1.9650 mL
	30 mM	0.0655 mL	0.3275 mL	0.6550 mL	1.6375 mL
	40 mM	0.0491 mL	0.2456 mL	0.4912 mL	1.2281 mL
	50 mM	0.0393 mL	0.1965 mL	0.3930 mL	0.9825 mL
	60 mM	0.0327 mL	0.1637 mL	0.3275 mL	0.8187 mL
	80 mM	0.0246 mL	0.1228 mL	0.2456 mL	0.6141 mL
	100 mM	0.0196 mL	0.0982 mL	0.1965 mL	0.4912 mL

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Voir tous les produits spécifiques à Isoform GSK-3

Voir tous les produits spécifiques à Isoform ERK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PPA24 Related Classifications

HY-163828 Related Classifications