(S)-PHA533533 |
Catalog No.GC27957
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 437982-89-3
Sample solution is provided at 25 µL, 10mM.
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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[1].
In Vitro, (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].
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].
References:
[1]. Vihma H, et al. Ube3a unsilencer for the potential treatment of Angelman syndrome. Nat Commun. 2024;15(1):5558. Published 2024 Jul 8.
| Cas No. | 437982-89-3 | SDF | |
| Chemical Name | Benzeneacetamide, N-(5-cyclopropyl-1H-pyrazol-3-yl)-α-methyl-4-(2-oxo-1-pyrrolidinyl)-, (αS)- | ||
| Canonical SMILES | C[C@H](C(NC1=NNC(C2CC2)=C1)=O)C3=CC=C(N4CCCC4=O)C=C3 | ||
| Formula | C19H22N4O2 | M.Wt | 338.40 |
| Solubility | DMSO : 100 mg/mL (295.51 mM; Need ultrasonic) | Storage | 4°C, protect from light |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9551 mL | 14.7754 mL | 29.5508 mL |
| 5 mM | 591 μL | 2.9551 mL | 5.9102 mL |
| 10 mM | 295.5 μL | 1.4775 mL | 2.9551 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)