Home Neuronal Signaling HDAC inhibitor Sodium Valproate (Valproic acid sodium)

연구용

Sodium Valproate (Valproic acid sodium) HDAC inhibitor

제품 번호: S1168

Valproic Acid sodium is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.
Sodium Valproate (Valproic acid sodium) HDAC inhibitor Chemical Structure

화학 구조

분자량: 166.19

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품질 관리 (Quality Control)

배치: 순도: 99.82%
99.82

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
HEK293 Function assay 1 mM Increase in protein disulfide isomerase level in HEK293 cells at 1 mM by immunoblot 17566732
HEK293 Function assay 1 mM Increase in GRP78 protein level in HEK293 cells at 1 mM by immunoblot 17566732
A549 Function assay 150 uM 24 hrs Inhibition of human HDAC in A549 cells assessed as increase in histone-H4 acetylation at 150 uM after 24 hrs by Western blot 18294844
GM15850 Function assay 400 uM 12 hrs Inhibition of HDAC in human GM15850 cells assessed as increase in total acetylated histone level at 400 uM after 12 hrs by Western blot analysis 16921367
PC12 Function assay 1 uM 24 hrs Induction of autophagy in rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 1 uM after 24 hrs by densitometric analysis 18391949
PC12 Function assay 1 uM 96 hrs Induction of autophagy in rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as soluble EGFP-HDQ74 clearance at 1 uM after 96 hrs by densitometric analysis 18391949
SK-N-MC Function assay 1 mM 48 hrs Induction of autophagy in human SK-N-MC cells expressing EGFP-HDQ74 assessed as reduction in EGFP-HDQ74 aggregation at 1 uM after 48 hrs by densitometric analysis 18391949
HL60 Function assay 1 mM 24 hrs Inhibition of HDAC in human HL60 cells assessed as increase in histone H3 acetylation at 1 mM after 24 hrs by Western blotting method 25304896
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 166.19 화학식

C8H15NaO2

 보관 (수령일로부터)
CAS 번호 1069-66-5 SDF 다운로드 원액 보관

동의어 Sodium valproate,NSC 93819,2-Propylpentanoic Acid Smiles CCCC(CCC)C(=O)[O-].[Na+]

용해도 (Solubility)

In vitro
배치:

Water : 100 mg/mL

DMSO : 33 mg/mL (198.56 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 33 mg/mL

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
HDAC
(Cell-free assay)
Autophagy
(Cell-free assay)
GABA receptor
(Cell-free assay)
notch1
시험관 내(In vitro)

Valproic acid acts through a distinct pathway that involves direct inhibition of histone deacetylase (IC(50) for HDAC1 = 0.4 mM). Valproic acid mimics the histone deacetylase inhibitor trichostatin A, causing hyperacetylation of histones in cultured cells. Valproic acid, like trichostatin A, also activates transcription from diverse exogenous and endogenous promoters. Valproic acid and trichostatin A have remarkably similar teratogenic effects in vertebrate embryos, while non-teratogenic analogues of valproic acid do not inhibit histone deacetylase and do not activate transcription.

Valproic acid induces proliferation of peroxisomes in the rodent liver. Valproic acid at a concentration of 1 mM induces relief of this repression by Gal4 fusions of N‐CoR, TR or PPARδ in a cell line expressing the ligand‐binding domain of PPARδ fused to the DNA‐binding domain of the glucocorticoid receptor (GR) together with a GR‐controlled reporter gene. Valproic acid induces accumulation of hyperacetylated histone and inhibits HDAC activity. Valproic acid induces a specific type of differentiation characterized by reduced proliferation, morphological alterations, marker gene expression and particularly the accumulation of the AP-2 transcription factor as a potential marker of neuronal or neural crest cell-like differentiation in F9 teratocarcinoma cells. Valproic acid impairs cell proliferation or survival as indicated by decreased incorporation of [3H]thymidine in F9 and P19 teratocarcinoma cells.

생체 내(In vivo)

Valproic acid delays growth of the primary tumors in the MT‐450 rat breast cancer model.

참조

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot Acetyl Histone H3 Active caspase-3 / PARP / Cleaved PARP acetyl-H4
S1168-WB1
28542253
Growth inhibition assay Cell viability
S1168-viability1
28498322

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT03919292 Recruiting
Solid Tumor Adult
Virginia Commonwealth University|Puma Biotechnology Inc.
 May 1 2019 Phase 1|Phase 2
NCT03681158 Completed
Epilepsy
Sanofi
 October 5 2018 Phase 1
NCT03112889 Completed
Glycogen Storage Disease Type V|McArdle Disease
University College London
 January 2015 Phase 2
NCT00139074 Terminated
Bipolar Disorder
AstraZeneca
 July 2005 Phase 4