Cat. No.: HY-167832

PT109

고객리뷰

Based on 1 Customer Validation

PT109 is an orally active, blood-brain barrier permeable multi-kinase inhibitor. By inhibiting PTBP1, PT109 promotes the switch of pyruvate kinase isoform from PKM2 to PKM1, thereby effectively inhibiting the proliferation and migration of glioblastoma multiforme and inducing its reprogramming into oligodendrocytes. PT109 also targets and regulates key signaling molecules such as JNK, SGK1, GSK3β to exert neuroprotective effects including promoting neurogenesis, inducing synapse formation and alleviating neuroinflammation. In Alzheimer's disease models, PT109 exhibits significant efficacy in improving spatial learning ability, along with excellent in vivo pharmacokinetic properties. PT109 can be used to investigate metabolic reprogramming of glioblastoma multiforme and neuroprotective mechanisms of Alzheimer's disease.

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Purity: 99.20%
CAS No.: 2059104-90-2
화학식: C₂₃H₃₁N₃OS₂
분자량:429.64

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PT109 Chemical Structure

CAS No.: 2059104-90-2

사이즈

가격

재고

수량

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

JNK1

0.143 μM (IC₅₀)

JNK2

0.831 μM (IC₅₀)

JNK3

0.285 μM (IC₅₀)

SGK1

1.34 μM (IC₅₀)

SGK2

5.6 μM (IC₅₀)

SGK3

26.4 μM (IC₅₀)

ROCK2

34 μM (IC₅₀)

MMP-9

MMP-2

COX-2

iNOS

PKM1

All JNK Isoforms :

All SGK Isoforms :

All ROCK Isoforms :

All MMP Isoforms :

All DNA/RNA Synthesis Isoforms :

All NF-κB Isoforms :

All COX Isoforms :

All NO Synthase Isoforms :

In Vitro

PT109 (10 μM; 24 h) significantly reduces the proportion of Ki67-positive (proliferative) human glioblastoma T98G and U251 cells^[1].
PT109 (10-20 μM; 24 h, 72 h) reduces the proteolytic activity and protein expression of MMP-2 and MMP-9 in a dose-dependent manner in T98G and U251 human glioblastoma cells, downregulates the expression of stem cell, astrocyte and neuron markers, while upregulating the expression of oligodendrocyte markers (MBP, MOG), induces morphological changes in T98G, U251 and U87 human glioblastoma cells^[1].
PT109 (10-20 μM; 72 h, 1-7 days) reduces the protein levels of PTBP1 and PKM2 in a dose- and time-dependent manner, while increasing the PKM1 level and the PKM1/PKM2 ratio, in human glioblastoma U251 cells, with the most significant effect observed at 20 μM for 7 days^[1].
PT109 (10 μM; 3 d) promotes the differentiation of C17.2 mouse neural stem cells into cholinergic neurons, upregulates the expression of neurogenesis markers and cholinergic markers, and does not induce astrocyte differentiation^[2].
PT109 (0.3-3 μM; 3 d) promotes synaptogenesis in primary rat hippocampal neurons and cortical neurons by upregulating the expression of the synaptogenesis marker Synapsin-1^[2].
PT109 (100 μg/mL; 10 h) exhibits favorable blood-brain barrier permeability in the in vitro PAMPA-BBB assay, indicating its potential for central nervous system exposure^[2].

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

Western Blot Analysis^[1]

Cell Line:

U251 human glioblastoma cell line
Concentration:

10, 20 μM (dose-response; 72 h); 20 μM (time-course; 1, 3, 7 days)
Incubation Time:

72 h; 1, 3, 7 days
Result:

Increased PKM1 protein levels and the PKM1/PKM2 ratio, and decreased PTBP1 and PKM2 protein levels, in a dose-dependent manner over 72 h. Decreased PTBP1 and PKM2 levels in a time-dependent manner, and increased PKM1 levels and the PKM1/PKM2 ratio in a time-dependent manner, over 7 days of treatment with 20 μM, with the most significant effects observed at 7 days (P<0.001 for PTBP1 reduction).

Cell Differentiation Assay^[2]

Cell Line:

C17.2 murine neural stem cells
Concentration:

10 μM
Incubation Time:

3 days
Result:

Increased the expression of Tuj-1 and MAP2 compared to vehicle control. Remarkably increased ChAT expression but showed no significant effect on GFAP expression relative to control.

In Vivo

PT109 (30-100 mg/kg; administered orally with diet daily; for 3-6 months) improves spatial learning and memory abilities, alleviates neuroinflammation, and downregulates the expression of phosphorylated JNK and Tau in APP/PS1 transgenic Alzheimer's disease mice^[2].

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

Animal Model:

APP/PS1 mice with Alzheimer's disease (male, 3 months old at study start, B6C3 background, Alzheimer's disease transgenic model)^[2]
Dosage:

30 mg/kg; 100 mg/kg
Administration:

oral; daily via diet; 3 or 6 months
Result:

Reduced Morris water maze escape latencies on day 5 (100 mg/kg, 6 months treatment).\n
Increased step-through test escape latency and reduced error frequency (100 mg/kg, 6 months treatment).\n
Significantly reduced number of activated microglia (Iba1-positive cells) and activated astrocytes (GFAP-positive cells) in brain cortex and hippocampus (30 mg/kg or 100 mg/kg, 3 or 6 months treatment).\nSignificantly reduced hippocampal levels of proinflammatory cytokines TNF-α, IL-1β, and IL-6 (30 mg/kg or 100 mg/kg, 6 months treatment).\n
Significantly reduced hippocampal levels of phosphorylated JNK (p-JNK) (30 mg/kg or 100 mg/kg, 6 months treatment).\n
Significantly reduced hippocampal and cortical levels of phosphorylated Tau (p-Tau, S396) (30 mg/kg or 100 mg/kg, 6 months treatment).

Chemical Information

CAS No. 2059104-90-2
Appearance Solid
분자량 429.64
화학식 C₂₃H₃₁N₃OS₂
Color Light yellow to yellow
SMILES

O=C(CCCCC1SSCC1)NC2CCC(CC2)NC3=CC=CC4=C3C=CN=C4
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 100 mg/mL (232.75 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

2.3275 mL

11.6376 mL

23.2753 mL

5 mM

0.4655 mL

2.3275 mL

4.6551 mL

10 mM

0.2328 mL

1.1638 mL

2.3275 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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 (5.82 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 (5.82 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 (5.82 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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Handling Instructions (2659 KB)

References

[1]. Yang Y, et al. PT109, a novel multi-kinase inhibitor suppresses glioblastoma multiforme through cell reprogramming: Involvement of PTBP1/PKM1/2 pathway. Eur J Pharmacol. 2022;920:174837. [Content Brief]

[2]. Chen Q, et al. Discovery of a novel small molecule PT109 with multi-targeted effects against Alzheimer's disease in vitro and in vivo. Eur J Pharmacol. 2020;883:173361. [Content Brief]

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

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	2.3275 mL	11.6376 mL	23.2753 mL	58.1882 mL
	5 mM	0.4655 mL	2.3275 mL	4.6551 mL	11.6376 mL
	10 mM	0.2328 mL	1.1638 mL	2.3275 mL	5.8188 mL
	15 mM	0.1552 mL	0.7758 mL	1.5517 mL	3.8792 mL
	20 mM	0.1164 mL	0.5819 mL	1.1638 mL	2.9094 mL
	25 mM	0.0931 mL	0.4655 mL	0.9310 mL	2.3275 mL
	30 mM	0.0776 mL	0.3879 mL	0.7758 mL	1.9396 mL
	40 mM	0.0582 mL	0.2909 mL	0.5819 mL	1.4547 mL
	50 mM	0.0466 mL	0.2328 mL	0.4655 mL	1.1638 mL
	60 mM	0.0388 mL	0.1940 mL	0.3879 mL	0.9698 mL
	80 mM	0.0291 mL	0.1455 mL	0.2909 mL	0.7274 mL
	100 mM	0.0233 mL	0.1164 mL	0.2328 mL	0.5819 mL

상품명:
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PT109

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Membrane Protein-targeted Compound Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

All JNK Isoforms

All SGK Isoforms

All ROCK Isoforms

All MMP Isoforms

All DNA/RNA Synthesis Isoforms

All NF-κB Isoforms

All COX Isoforms

All NO Synthase Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

PT109 Related Classifications

HY-167832 Related Classifications