2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. CDK E1/E2/E3 Enzyme
  4. (S)-PHA533533

(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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(S)-PHA533533

(S)-PHA533533 構造式

CAS 番号 : 437982-89-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1452 在庫あり
Solution
10 mM * 1 mL in DMSO USD 1452 在庫あり
Solid
1 mg $525 在庫あり
5 mg $1320 在庫あり
10 mg $1850 在庫あり
25 mg $2960 在庫あり
50 mg $4000 在庫あり
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200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

Other Forms of (S)-PHA533533:

(S)-PHA533533 関連抗体

Top Publications Citing Use of Products

CDK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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製品説明

(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[1].

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]
A2780 IC50
744 nM
Compound: 13 (table 2)
Inhibitory concentration towards Human ovarian carcinoma cell line A2780
Inhibitory concentration towards Human ovarian carcinoma cell line A2780
[PMID: 15828833]
A2780 IC50
800 nM
Compound: 13 (table 2)
Inhibitory concentration towards human ovarian carcinoma cell line A2780
Inhibitory concentration towards human ovarian carcinoma cell line A2780
[PMID: 15828833]
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]
体外実験

(S)-PHA533533 (1 μM; 72 h) potently activates paternal Ube3a expression in primary cortical neurons from Ube3am+/pYFP mice[1].
(S)-PHA533533 (72 h) activates paternal Ube3a expression in primary cortical neurons from Ube3am+/pYFP mice, with an EC50 of 0.54 μM, an EMAX 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 Ube3am+/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.

(S)-PHA533533 関連抗体
Parmacokinetics
Species Dose Route CL Cmax AUC
Mice[1] 10 mg/kg p.o. 5.8 mL/min/kg 21 μM 96 μM·h
体内実験

(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 (Ube3am-/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.
分子量

338.40

分子式

C19H22N4O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light

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

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
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 (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.

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  • Dilution Calculator

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

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一般には略語で表示されます：C1V1 = C2V2

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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 (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.

    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 (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.

    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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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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 (protect from 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.
純度とドキュメンテーション
参考文献

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 (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.

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 Related Classifications

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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

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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:

(S)-PHA533533437982-89-3CDKE1/E2/E3 EnzymeCyclin dependent kinaseE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseCDK5neuronsblood-brain barrierCDK2/cyclin ECDK2/cyclin AAngelman syndromeCDK2CDK5/p25 complexesInhibitorinhibitorinhibit

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製品名:
(S)-PHA533533
製品番号:
HY-162683
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