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  1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. Nexturastat A

Nexturastat A 是一種有效的選擇性 HDAC6 抑制劑。Nexturastat A 對 HDAC6 具有抑制作用,IC50 為 5 nM。Nexturastat A 可用于多發(fā)性骨髓瘤 (MM) 的研究。

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Nexturastat A Chemical Structure

Nexturastat A Chemical Structure

CAS No. : 1403783-31-2

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10 mM * 1 mL in DMSO ¥1727
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1 mg ¥780
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5 mg ¥2300
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10 mg ¥3900
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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Nexturastat A is a potent, selective HDAC6 inhibitor. Nexturastat A has inhibitory for HDAC6 with an IC50 of 5 nM. Nexturastat A can be used for the research of multiple myeloma (MM)[1][2].

IC50 & Target[1]

HDAC6

5.02 nM (IC50)

HDAC8

0.954 μM (IC50)

HDAC1

3.02 μM (IC50)

HDAC7

4.46 μM (IC50)

HDAC11

5.14 μM (IC50)

HDAC3

6.68 μM (IC50)

HDAC9

6.72 μM (IC50)

HDAC2

6.92 μM (IC50)

HDAC10

7.57 μM (IC50)

HDAC4

9.39 μM (IC50)

HDAC5

11.7 μM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
697 IC50
401 nM
Compound: Nexturastat
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
[PMID: 31710483]
B16 GI50
14.3 μM
Compound: 5g, Nexturastat A
Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay
Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay
[PMID: 23009203]
MCF7 IC50
1.4 μM
Compound: Nexturastat A
Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay
[PMID: 29317150]
MM1.S IC50
1.76 μM
Compound: Nexturastat
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
MV4-11 IC50
1.68 μM
Compound: Nexturastat
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
MV4-11 IC50
1.68 μM
Compound: Nexturastat
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
Sf9 IC50
0.005 μM
Compound: NextA
Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s
Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s
[PMID: 31414801]
Sf9 IC50
2.86 μM
Compound: NextA
Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi
Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi
[PMID: 31414801]
Sf9 IC50
25 nM
Compound: Nexturastat
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
[PMID: 31710483]
Sf9 IC50
3020 nM
Compound: 5g, Nexturastat A
Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
[PMID: 23009203]
Sf9 IC50
5.02 nM
Compound: 5g, Nexturastat A
Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate
[PMID: 23009203]
體外研究
(In Vitro)

Nexturastat A (5 g) 對 HDAC6 具有抑制作用,IC50 值為 0.005 μM[1]
Nexturastat A (0-10 μM;24 小時) 對 HDAC62 具有底物選擇性[1]
Nexturastat A 對 B16 鼠黑色素瘤細(xì)胞具有抗增殖活性,IC50 值為 14.3 μM[1]。
Nexturastat A (NexA)? (0-40 μM;48 小時) 抑制人 MM 細(xì)胞的活力并誘導(dǎo) G1 期阻滯[2]。
Nexturastat A (0,30,40 μM;48 h) 通過轉(zhuǎn)錄激活 p21 啟動子促進(jìn) MM 細(xì)胞凋亡[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: B16 murine melanoma cells
Concentration: 0-10 μM
Incubation Time: 24 h
Result: Increased the level of acetyl α-tubulin levels in a dose-dependent.

Cell Viability Assay[2]

Cell Line: RPMI-8226 and U266 cells
Concentration: 0-40 μM
Incubation Time: 48 h
Result: Impaired multiple myeloma (MM) cells viability in a dose- and time-dependent manner.

Apoptosis Analysis[2]

Cell Line: RPMI-8226 and U266 cells
Concentration: 0, 30, 40 μM
Incubation Time: 48 h
Result: Induced cell apoptosis in human MM cells.

RT-PCR[2]

Cell Line: RPMI-8226 and U266 cells
Concentration: 30 μM
Incubation Time: 48 h
Result: Increased the levels of p21 mRNA in RPMI-8226 and U266 cells.
體內(nèi)研究
(In Vivo)

Nexturastat A (NexA)? (每兩天一次,20 天一次) 抑制小鼠 MM 異種移植模型中的腫瘤生長[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

341.40

Formula

C19H23N3O3

CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實驗: 

DMSO 中的溶解度 : ≥ 56 mg/mL (164.03 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.9291 mL 14.6456 mL 29.2912 mL
5 mM 0.5858 mL 2.9291 mL 5.8582 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.32 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.32 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL  μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
連續(xù)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9291 mL 14.6456 mL 29.2912 mL 73.2279 mL
5 mM 0.5858 mL 2.9291 mL 5.8582 mL 14.6456 mL
10 mM 0.2929 mL 1.4646 mL 2.9291 mL 7.3228 mL
15 mM 0.1953 mL 0.9764 mL 1.9527 mL 4.8819 mL
20 mM 0.1465 mL 0.7323 mL 1.4646 mL 3.6614 mL
25 mM 0.1172 mL 0.5858 mL 1.1716 mL 2.9291 mL
30 mM 0.0976 mL 0.4882 mL 0.9764 mL 2.4409 mL
40 mM 0.0732 mL 0.3661 mL 0.7323 mL 1.8307 mL
50 mM 0.0586 mL 0.2929 mL 0.5858 mL 1.4646 mL
60 mM 0.0488 mL 0.2441 mL 0.4882 mL 1.2205 mL
80 mM 0.0366 mL 0.1831 mL 0.3661 mL 0.9153 mL
100 mM 0.0293 mL 0.1465 mL 0.2929 mL 0.7323 mL
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.

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產(chǎn)品名稱:
Nexturastat A
目錄號:
HY-16699
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