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  1. Cell Cycle/DNA Damage Apoptosis
  2. CDK Apoptosis
  3. NVP-2

NVP-2 是一種有效且具有選擇性的 ATP 競爭性細(xì)胞周期蛋白依賴性激酶 9 (CDK9) 探針,可抑制 CDK9/CycT 活性,IC50 值為 0.514 nM。NVP-2 對 CDK1/CycB,CDK2/CycA 和 CDK16/CycY 激酶具有抑制作用,其 IC50 值分別為 0.584 μM,0.706 μM 和 0.605 μM。NVP-2誘導(dǎo)細(xì)胞凋亡 (apoptosis)。

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NVP-2 Chemical Structure

NVP-2 Chemical Structure

CAS No. : 1263373-43-8

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10 mM * 1 mL in DMSO ¥1693
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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 33 篇科研文獻(xiàn)

WB

    NVP-2 purchased from MCE. Usage Cited in: Cell Rep. 2021 Mar 16;34(11):108870.  [Abstract]

    NVP-2 treatment suppresses RNA polymerase II (RNAPII) CTD pSer2, pAKT, MYC, and MCL-1 levels and augments PARP cleavage in primary MCL patient samples (Pt0448, Pt1888) in a dose-dependent fashion.

    NVP-2 purchased from MCE. Usage Cited in: Neoplasia. 2019 Jul;21(7):713-720.  [Abstract]

    LNCaP cells were treated with DMSO or increasing dose of NVP2 for 24 hours and samples are analyzed using western blotting. Densitometry is used to evaluate the abundance of each protein.

    NVP-2 purchased from MCE. Usage Cited in: Cell. 2018 Sep 20;175(1):171-185.e25.  [Abstract]

    WB analysis of MV4-11 cells treated with BTX161 (6 hr), iCDK9 (4 hr), or THZ1 (4 hr) at the indicated concentrations in different combinations as indicated. PP2Ac is a loading control.
    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 μM, 0.706 μM, and 0.605 μM, respectively. NVP-2 induces cell apoptosis.[1]

    IC50 & Target

    CDK9

    0.5 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Jurkat GI50
    < 0.16 μM
    Compound: NVP-2
    Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    [PMID: 32129996]
    L02 GI50
    28.33 μM
    Compound: NVP-2
    Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    [PMID: 32129996]
    MCF7 GI50
    43.36 μM
    Compound: NVP-2
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    [PMID: 32129996]
    MDA-MB-231 GI50
    < 0.16 μM
    Compound: NVP-2
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay
    [PMID: 32129996]
    Sf9 IC50
    > 10 μM
    Compound: NVP-2
    Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay
    Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay
    [PMID: 32129996]
    Sf9 IC50
    0.002 μM
    Compound: NVP-2
    Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay
    Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay
    [PMID: 32129996]
    Sf9 IC50
    3.46 μM
    Compound: NVP-2
    Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay
    Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay
    [PMID: 32129996]
    體外研究
    (In Vitro)

    NVP-2 has an anti-proliferation of leukemia cells, inhibits KOPT-K1, Jurkat, P12-ICHIKAWA, DU.528, MOLT 16, HSB-2, PF-382, SKW-3, SUP-T11, DND-41 and HPB-ALL cells with IC50 values of 0.1688 μM, 0.1233? μM,0.5736? μM,0.1575 μM, 0.1620 μM,0.1585 μM, 0.1808 μM, 0.2589 μM, 0.0918 μM and 0.3023 μM, respectively[1].
    ? NVP-2 (250 nM-1 μM; 6 hours) engages CDK9 in wildtype and?CRBN?/??MOLT4 cells at all concentrations, while CDK2 and CDK7 are unaffected[1].
    ? NVP-2 (0-10 nM; 72 hours) exhibits CRBN-dependent anti-proliferative and pro-apoptotic effects in MOLT4 cells, displays an IC50 value of 9 nM[1].
    ? NVP-2 (250 nM; 24 hours) induces cell apoptosis in MOLT4 cells, upregulates caspase-3 and γH2A.X expression. However, while the compound washout significantly reduces the degree of apoptosis induced by NVP-2[1].

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

    Cell Viability Assay[1]

    Cell Line: Leukemia cell lines
    Concentration: 0.1233 μM-0.5736 μM
    Incubation Time: 72 hours
    Result: Inhibited Leukemia cell lines viabity.

    Western Blot Analysis[1]

    Cell Line: Wildtype and?CRBN?/??MOLT4 cells
    Concentration: 1 μM; 500 nM; 250 nM
    Incubation Time: 6 hours
    Result: Degrade CDK9 ?sub-stoichiometrically at all concentrations.

    Apoptosis Analysis[1]

    Cell Line: Wildtype and?CRBN?/??MOLT4 cells
    Concentration: 250 nM
    Incubation Time: 24 hours
    Result: Induced cell apoptosis in cells and wash outed the compound relieved NVP-2-induced cell apoptosis.

    Cell Proliferation Assay[1]

    Cell Line: MOLT4 cells
    Concentration: 0-10 nM
    Incubation Time: 72 hours
    Result: Exhibited anti-proliferative effects in MOLT4 cells.
    分子量

    513.07

    Formula

    C27H37ClN6O2

    CAS 號
    性狀

    固體

    顏色

    White to yellow

    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 : ≥ 100 mg/mL (194.91 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 1.9491 mL 9.7453 mL 19.4905 mL
    5 mM 0.3898 mL 1.9491 mL 3.8981 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 (4.87 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 (4.87 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

    純度: 99.60%

    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 1.9491 mL 9.7453 mL 19.4905 mL 48.7263 mL
    5 mM 0.3898 mL 1.9491 mL 3.8981 mL 9.7453 mL
    10 mM 0.1949 mL 0.9745 mL 1.9491 mL 4.8726 mL
    15 mM 0.1299 mL 0.6497 mL 1.2994 mL 3.2484 mL
    20 mM 0.0975 mL 0.4873 mL 0.9745 mL 2.4363 mL
    25 mM 0.0780 mL 0.3898 mL 0.7796 mL 1.9491 mL
    30 mM 0.0650 mL 0.3248 mL 0.6497 mL 1.6242 mL
    40 mM 0.0487 mL 0.2436 mL 0.4873 mL 1.2182 mL
    50 mM 0.0390 mL 0.1949 mL 0.3898 mL 0.9745 mL
    60 mM 0.0325 mL 0.1624 mL 0.3248 mL 0.8121 mL
    80 mM 0.0244 mL 0.1218 mL 0.2436 mL 0.6091 mL
    100 mM 0.0195 mL 0.0975 mL 0.1949 mL 0.4873 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:
    NVP-2
    目錄號:
    HY-12214A
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