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首页-小分子抑制剂&激动剂-Others-Other Targets-(S)-PHA533533
(S)-PHA533533

Chemical Structure : (S)-PHA533533

CAS No.: 437982-89-3

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(S)-PHA533533 ((S)-PHA 533533)

货号: PC-22640Not For Human Use, Lab Use Only.

(S)-PHA533533 is a potent, small molecule unsilencer of paternal UBE3A in mouse primary neurons with EC50 of 0.54 uM, Emax=80%, effectively downregulates Ube3a-ATS/UBE3A ATS and epigenetically unsilences paternal Ube3a/UBE3A in both mouse and human neuron.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

(S)-PHA533533 is a potent, small molecule unsilencer of paternal UBE3A in mouse primary neurons with EC50 of 0.54 uM, Emax=80%, effectively downregulates Ube3a-ATS/UBE3A ATS and epigenetically unsilences paternal Ube3a/UBE3A in both mouse and human neuron.
(S)-PHA533533 is a compound previously developed as a cyclin-dependentkinase 2 (CDK2) inhibitor.
(S)-PHA533533 downregulate a long non-coding anti sense (UBE3A-ATS) transcript and unsilences paternal Ube3a in primary neurons derived from AS model mice (Ube3am–/p+).
(S)-PHA533533 downregulated the Ube3a-ATS similarly to topotecan, significantly increased Ube3a mRNA and protein levels in WT neurons.
The unsilencing of paternal Ube3a by (S)-PHA533533 occurs independently from its known CDK2/CKD5 targets and topoi somerase I inhibition.
Peripheral delivery of (S)-PHA533533 (2mg/kg) can produce brain-wide unsilencing of paternal Ube3a in AS model mice.
(S)-PHA533533 reduces the expression on UBE3A ATS in human ASdel1-0ΔI-P neurons with IC50 of 0.42 uM, EC50 of 0.59 uM for for unsilencing paternal UBE3A.
(S)-PHA533533 downregulates the UBE3A antisense (UBE3A-ATS) transcript and increases paternal UBE3A mRNA in neurons derived from patients with Angelman syndrome.

物理化学性质&存储条件

分子量 338.41
分子式 C19H22N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(4-(2-oxopyrrolidin-1-yl)phenyl)propanamide

参考文献

1. Vihma H, et al. Nat Commun. 2024 Jul 8;15(1):5558.

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