Home Epigenetics HDAC inhibitor Tubastatin A Hydrochloride

연구용

Tubastatin A Hydrochloride HDAC6 Inhibitor

제품 번호: S2627

Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
Tubastatin A Hydrochloride HDAC inhibitor Chemical Structure

화학 구조

분자량: 371.86

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품질 관리 (Quality Control)

배치: 순도: 99.30%
99.30

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
neuron cultures Kinase assay 2.5 μM DMSO induces α-tubulin hyperacetylation
neuron cultures Function assay ~10 μM DMSO protects against glutathione depletion-induced oxidative stress
134/04 Function assay 7.5 µM impairs myotube formation
C2C12 Function assay 7.5 µM impairs myotube formation
HaCaT keratinocytes Function assay 10 μM blocks arsenite from inducing Nrf2 protein translation
JURL-MK1 Function assay 10 μM enhances cell adhesivity to fibronectin
CML-T1 Function assay 10 μM enhances cell adhesivity to fibronectin
K562 Function assay 10 μM enhances cell adhesivity to fibronectin
HL-60 Function assay 10 μM enhances cell adhesivity to fibronectin
KMCH Growth inhibitory assay ~10 μM decreases proliferation and anchorage-independent growth
THP-1 Function assay ~10 μM inhibits TNF-α and IL-6 secretion
RAW 264.7 Function assay ~10 μM attenuates NO production
HT3 Function assay ~5 μM DMSO induces the differential α-tubulin acetylation
SiHa Function assay ~5 μM DMSO induces the differential α-tubulin acetylation
CaSki Function assay ~5 μM DMSO induces the differential α-tubulin acetylation
SiHa Function assay ~5 μM DMSO inhibits Thapsigargin- or EGF-induced SOCE activation
CaSki Function assay ~5 μM DMSO inhibits Thapsigargin- or EGF-induced SOCE activation
MCF-7 Growth inhibitory assay 30 μM DMSO IC50=15 μM
MCF-7 Function assay 30 μM DMSO increases the microtubule acetylation level.
MCF-7 Function assay 30 μM DMSO stabilizes microtubules against cold-induced depolymerization
MCF-7 Function assay 15 μM DMSO stabilizes microtubules against nocodazole-induced disassembly
MCF-7 Function assay 30 μM DMSO alteres the assembly dynamics of interphase microtubules
MCF-7 Function assay 30 μM DMSO increases the binding of HDAC6 with interphase microtubules
PC12 Function assay ~3 μM DMSO up-regulates anti-oxidative gene expression related to transcription factor XBP1s
PC12 Growth inhibitory assay ~3 μM DMSO reverse H2O2-induced growth inhibition
HEK293T Function assay ~3 μM DMSO up-regulated XBP1s protein level
HEK293T Function assay ~3 μM DMSO delays XBP1s protein degradation via acetylation-mediated proteasomal degradation
Huh7 Function assay ~5 μM DMSO suppresses proliferation of hepatitis C virus replicon with EC50 = 0.3 μM
SKMEL21 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation
SKMEL103 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation
SKMEL28 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation
WM164 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation
WM1361a Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation
WM1366 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation
WM793 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation
WM35 Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation
WM983a Growth inhibitory assay ~500 nM DMSO inhibits cell proliferation
WM793 Function assay ~6 μM DMSO induce G1 arrest
WM164 Function assay ~6 μM DMSO induce G1 arrest
WM983a Function assay ~6 μM DMSO induce G1 arrest
WM164 Function assay ~3 μM DMSO augments expression of MHC class I and melanoma associated antigens
WM983a Function assay ~3 μM DMSO augments expression of MHC class I and melanoma associated antigens
IPC298 Function assay ~3 μM DMSO augments expression of MHC class I and melanoma associated antigens
SKMEL30 Function assay ~3 μM DMSO augments expression of MHC class I and melanoma associated antigens
TCa83 Function assay induces PTEN expression and membrane translocation
293T Function assay ~2 μg/ml induces PTEN expression and membrane translocation
SACC-83 Function assay ~2 μg/ml induces PTEN expression and membrane translocation
293T Function assay ~2 μg/ml induces PTEN acetylation at K163
U-87 MG Function assay ~2 μg/ml inhibits the migration and invasion
U-87 MG Function assay ~10 μM inhibits AKT phosphorylation
U-87 MG Growth inhibitory assay ~10 μM inhibits cell growth
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 371.86 화학식

C20H21N3O2.HCl

 보관 (수령일로부터)
CAS 번호 1310693-92-5 SDF 다운로드 원액 보관

용해도 (Solubility)

In vitro
배치:

DMSO : 100 mg/mL (268.91 mM) 50°C 수조에서 가온; 초음파 처리;
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

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
HDAC6
(Cell-free assay)
15 nM
HDAC8
(Cell-free assay)
854 nM
시험관 내(In vitro)
Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. In homocysteic acid (HCA) induced neurodegeneration assays, Tubastatin A displays dose-dependent protection against HCA-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM. At 100 ng/mL Tubastatin A increases Foxp3+ T-regulatory cells (Tregs) suppression of T cell proliferation in vitro. Tubastatin A treatment in C2C12 cells would lead to myotube formation impairment when alpha-tubulin is hyperacetylated early in the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyeperacetylated in myotubes. A recent study indicates that Tubastatin A treatment increases cell elasticity as revealed by atomic force microscopy (AFM) tests without exerting drastic changes to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L.
키나아제 분석
Enzyme Inhibition Assays
Enzyme inhibition assays are performed by the Reaction Biology Corporation, Malvern, PA, using the Reaction Biology HDAC Spectrum platform. (www.reactionbiology.com) The HDAC1, 2, 4, 5, 6, 7, 8, 9, 10, and 11 assays use isolated recombinant human protein; HDAC3/NcoR2 complex is used for the HDAC3 assay. Substrate for HDAC1, 2, 3, 6, 10, and 11 assays is a fluorogenic peptide from p53 residues 379-382 (RHKKAc); substrate for HDAC8 is fluorogenic diacyl peptide based on residues 379-382 of p53 (RHKAcKAc). Acetyl-Lys (trifluoroacetyl)-AMC substrate is used for HDAC4, 5, 7, and 9 assays. Tubastatin A is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 30 μM. Control Compound Trichostatin A (TSA) is tested in a 10-dose IC50 with 3-fold serial dilution starting at 5 μM. IC50 values are extracted by curve-fitting the dose/response slopes.
생체 내(In vivo)
Daily treatment of Tubastatin A at 0.5mg/kg inhibits HDAC6 to promote Tregs suppressive activity in mouse models of inflammation and autoimmunity, including multiple forms of experimental colitis and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/22446682/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot EGFR / p-AKT / AKT / p-ERK / ERK
S2627-WB1
29665050
Immunofluorescence α-tubulin / Acetylated tubulin HDAC6
S2627-IF1
23798680