Art. -Nr.: HY-162683

(S)-PHA533533

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(S)-PHA533533 is a CDK2 and CDK5 inhibitor with blood-brain barrier permeability, with IC₅₀ values of 37 nM and 55 nM, respectively. (S)-PHA533533 effectively restores UBE3A expression by downregulating UBE3A-ATS and relieving the epigenetic silencing of paternal UBE3A in mature neurons. (S)-PHA533533 can be used for the research of Angelman syndrome.

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Reinheit: 98.27%
CAS. Nr.: 437982-89-3
Formel: C₁₉H₂₂N₄O₂
Molecular Weight:338.40

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

(S)-PHA533533 Chemical Structure

CAS. Nr.: 437982-89-3

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.8 μM Compound: 1, PHA-533533	Antiproliferative activity against human A2780 cells Antiproliferative activity against human A2780 cells	[PMID: 16616492]
HCT-116	IC₅₀	1354 nM Compound: 13 (table 2)	Inhibitory concentration towards HCT 116 human colon cancer cell line Inhibitory concentration towards HCT 116 human colon cancer cell line	[PMID: 15828833]
HT-29	IC₅₀	639 nM Compound: 13 (table 2)	Inhibitory concentration towards human colon cancer HT-29 cell line Inhibitory concentration towards human colon cancer HT-29 cell line	[PMID: 15828833]

In Vitro

(S)-PHA533533 (1 μM; 72 h) potently activates paternal Ube3a expression in primary cortical neurons from Ube3a^m+/pYFP mice^[1].
(S)-PHA533533 (72 h) activates paternal Ube3a expression in primary cortical neurons from Ube3a^m+/pYFP mice, with an EC₅₀ of 0.54 μM, an E_MAX of 80.02% paternal UBE3A-YFP-positive neurons, and a CC₅₀ of 2.98 μM^[1].
(S)-PHA533533 (1 μM; 72 h) activates paternal Ube3a expression in primary cortical neurons derived from Ube3a^m+/pYFP mice, and this process is independent of the inhibition of CDK2, CDK5 and TOP1^[1].
(S)-PHA533533 (72 h) downregulates UBE3A-ATS and relieves the silencing of paternal UBE3A in forebrain cortical neurons derived from ASdel1-0ΔI-P human induced pluripotent stem cells, with an EC₅₀ of 0.59 μM for UBE3A induction and an IC₅₀ of 0.42 μM for UBE3A-ATS downregulation^[1].

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

Parmacokinetics

Species	Dose	Route	CL	C_max	AUC
Mice^[1]	10 mg/kg	p.o.	5.8 mL/min/kg	21 μM	96 μM·h

In Vivo

(S)-PHA533533 (2 mg/kg; i.p.; single injection) produces brain-wide unsilencing of paternal Ube3a, significantly increasing Ube3a mRNA and UBE3A protein levels in neurons of Angelman syndrome model mice^[1].

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

Animal Model:

C57BL/6J (Ube3a^m-/p+ Angelman syndrome model, postnatal day 11)^[1]
Dosage:

2 mg/kg
Administration:

i.p.; single injection
Result:

Significantly increased Ube3a mRNA levels in all examined brain regions (olfactory bulb, cortex and hippocampus, subcortical tissues, cerebellum) compared to saline-treated control AS mice.
Reached Ube3a mRNA levels measured in saline-treated wild-type mice in the olfactory bulb.
Widespread reinstated UBE3A protein throughout the brain, with increased UBE3A signal detected in all NeuN-positive mature neurons across multiple brain regions.

Chemical Information

CAS. Nr. 437982-89-3
Appearance Solid
Molecular Weight 338.40
Formel C₁₉H₂₂N₄O₂
Color White to off-white
SMILES

C[C@H](C(NC1=NNC(C2CC2)=C1)=O)C3=CC=C(N4CCCC4=O)C=C3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (295.51 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

2.9551 mL

14.7754 mL

29.5508 mL

5 mM

0.5910 mL

2.9551 mL

5.9102 mL

10 mM

0.2955 mL

1.4775 mL

2.9551 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (7.39 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 (7.39 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 (7.39 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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)

Verweise

[1]. Vihma H, et al. Ube3a unsilencer for the potential treatment of Angelman syndrome. Nat Commun. 2024;15(1):5558. Published 2024 Jul 8. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9551 mL	14.7754 mL	29.5508 mL	73.8771 mL
	5 mM	0.5910 mL	2.9551 mL	5.9102 mL	14.7754 mL
	10 mM	0.2955 mL	1.4775 mL	2.9551 mL	7.3877 mL
	15 mM	0.1970 mL	0.9850 mL	1.9701 mL	4.9251 mL
	20 mM	0.1478 mL	0.7388 mL	1.4775 mL	3.6939 mL
	25 mM	0.1182 mL	0.5910 mL	1.1820 mL	2.9551 mL
	30 mM	0.0985 mL	0.4925 mL	0.9850 mL	2.4626 mL
	40 mM	0.0739 mL	0.3694 mL	0.7388 mL	1.8469 mL
	50 mM	0.0591 mL	0.2955 mL	0.5910 mL	1.4775 mL
	60 mM	0.0493 mL	0.2463 mL	0.4925 mL	1.2313 mL
	80 mM	0.0369 mL	0.1847 mL	0.3694 mL	0.9235 mL
	100 mM	0.0296 mL	0.1478 mL	0.2955 mL	0.7388 mL

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(S)-PHA533533

MCE Bioactive Compound Library

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

(S)-PHA533533 Related Classifications

HY-162683 Related Classifications