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  2. Epigenetics
  3. Histone Methyltransferase
  4. UNC0642

UNC0642是有效，選擇性的賴氨酸甲基轉(zhuǎn)移酶 G9a 和 GLP 抑制劑， 抑制 G9a 的IC50 值小于2.5 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

UNC0642 Chemical Structure

UNC0642 Chemical Structure

CAS No. : 1481677-78-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥902
In-stock
1 mg ￥340
In-stock
5 mg ￥750
In-stock
10 mg ￥1194
In-stock
50 mg ￥3850
In-stock
100 mg ￥5518
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

    UNC0642 purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 Aug;40(8):1076-1084.  [Abstract]

    UNC0642 suppresses the activity of G9a protein according to detection of the level of H3K9me2. T24 and J82 cells are treated with UNC0642 for 24 h at the indicated concentration.

    UNC0642 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.  [Abstract]

    H3K9Me2, PTEN, p-AKT, and AKT expression levels are measured in PC9/ER xenograft tumor tissues. β-actin is used as a loading control.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC50 of <2.5 nM for G9a.

    IC50 & Target

    EHMT2/G9a/KMT1C

     

    EHMT1/GLP/KMT1D

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-431 IC50
    3.38 μM
    Compound: UNC0642
    Antiproliferative activity against human A-431 cells measured after 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells measured after 72 hrs by MTT assay
    		[PMID: 34847495]
    HCT-116 IC50
    5.01 μM
    Compound: UNC0642
    Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay
    		[PMID: 34847495]
    HeLa IC50
    1.74 μM
    Compound: UNC0642
    Antiproliferative activity against human HeLa cells measured after 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells measured after 72 hrs by MTT assay
    		[PMID: 34847495]
    HepG2 IC50
    2.69 μM
    Compound: UNC0642
    Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay
    		[PMID: 34847495]
    HT-29 IC50
    1.35 μM
    Compound: UNC0642
    Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay
    		[PMID: 34847495]
    K562 IC50
    0.92 μM
    Compound: UNC0642
    Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay
    Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay
    		[PMID: 34847495]
    L02 IC50
    3.23 μM
    Compound: UNC0642
    Cytotoxicity against human HL7702 cells measured after 72 hrs by MTT assay
    Cytotoxicity against human HL7702 cells measured after 72 hrs by MTT assay
    		[PMID: 34847495]
    MDA-MB-231 IC50
    110 nM
    Compound: 7, UNC0642
    Inhibition of lysine methyltransferase G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
    Inhibition of lysine methyltransferase G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
    		[PMID: 24102134]
    MDA-MB-231 EC50
    16700 nM
    Compound: 7, UNC0642
    Cytotoxicity against human MDA-MB-231 cells after 48 hrs by Alamar Blue assay
    Cytotoxicity against human MDA-MB-231 cells after 48 hrs by Alamar Blue assay
    		[PMID: 24102134]
    MDA-MB-231 IC50
    3.23 μM
    Compound: UNC0642
    Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay
    		[PMID: 34847495]
    PANC-1 EC50
    3500 nM
    Compound: 7, UNC0642
    Cytotoxicity against human PANC1 cells after 48 hrs by Alamar Blue assay
    Cytotoxicity against human PANC1 cells after 48 hrs by Alamar Blue assay
    		[PMID: 24102134]
    PANC-1 IC50
    40 nM
    Compound: 7, UNC0642
    Inhibition of lysine methyltransferase G9a in human PANC1 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
    Inhibition of lysine methyltransferase G9a in human PANC1 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
    		[PMID: 24102134]
    PC-3 IC50
    130 nM
    Compound: 7, UNC0642
    Inhibition of lysine methyltransferase G9a in human PC3 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
    Inhibition of lysine methyltransferase G9a in human PC3 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
    		[PMID: 24102134]
    PC-3 EC50
    8900 nM
    Compound: 7, UNC0642
    Cytotoxicity against human PC3 cells after 48 hrs by Alamar Blue assay
    Cytotoxicity against human PC3 cells after 48 hrs by Alamar Blue assay
    		[PMID: 24102134]
    U2OS IC50
    130 nM
    Compound: 7, UNC0642
    Inhibition of lysine methyltransferase G9a in human U2OS cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
    Inhibition of lysine methyltransferase G9a in human U2OS cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
    		[PMID: 24102134]
    U2OS EC50
    6000 nM
    Compound: 7, UNC0642
    Cytotoxicity against human U2OS cells after 48 hrs by Alamar Blue assay
    Cytotoxicity against human U2OS cells after 48 hrs by Alamar Blue assay
    		[PMID: 24102134]
    體外研究
    (In Vitro)

    UNC0642 顯示出高體外 和細(xì)胞效力、低細(xì)胞毒性和出色的選擇性。UNC0642 與肽底物競(jìng)爭(zhēng)，與輔助因子 SAM 不競(jìng)爭(zhēng)。UNC0642 的Ki測(cè)定為3.7±1 nM。UNC0642 對(duì) GLP 表現(xiàn)出高體外效力 (IC50< 2.5 nM)，類似于 G9a。UNC0642 在廣泛的激酶、GPCR、轉(zhuǎn)運(yùn)蛋白和離子通道中對(duì) G9a 和 GLP 的選擇性超過(guò) 300 倍。UNC0642 在降低 H3K9me2 標(biāo)記方面表現(xiàn)出高效力，細(xì)胞毒性低，并且在許多細(xì)胞系中功能效力和細(xì)胞毒性的良好分離。它降低了胰腺癌細(xì)胞系 PANC-1 細(xì)胞的克隆形成[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    單次腹膜內(nèi) (IP) 注射 (5 mg/kg) UNC0642 可產(chǎn)生 947 ng/mL 的血漿 Cmax (最大濃度) 和 1265 小時(shí)的 AUC (曲線下面積) *ng/mL[1]。

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

    546.70

    Formula

    C29H44F2N6O2
    CAS 號(hào)
    性狀

    固體

    顏色

    Off-white to light yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)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(shí)驗(yàn)： 

    DMSO 中的溶解度 : 50 mg/mL (91.46 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.8292 mL 9.1458 mL 18.2916 mL
    5 mM 0.3658 mL 1.8292 mL 3.6583 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)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(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)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(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.57 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。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.57 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。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)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(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)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(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)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: 99.92%

    參考文獻(xiàn)
    Cell Assay
    [1]

    MDA-MB-231, PC3, and U2OS cells are treated with inhibitors (UNC0642) for 48 h. Cell viability assays are performed by incubating cells with 0.1 mg/mL of resazurin for 3 – 4 h. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm. In-cell western assay is performed as described previously[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: Standard PK studies are performed using male Swiss albino mice. Plasma and brain concentrations are measured at 0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h following a single IP injection of UNC0642 at 5 mg/kg. The compound concentration at each time point in plasma or brain is the average value from 3 test animals[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?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 1.8292 mL 9.1458 mL 18.2916 mL 45.7289 mL
    5 mM 0.3658 mL 1.8292 mL 3.6583 mL 9.1458 mL
    10 mM 0.1829 mL 0.9146 mL 1.8292 mL 4.5729 mL
    15 mM 0.1219 mL 0.6097 mL 1.2194 mL 3.0486 mL
    20 mM 0.0915 mL 0.4573 mL 0.9146 mL 2.2864 mL
    25 mM 0.0732 mL 0.3658 mL 0.7317 mL 1.8292 mL
    30 mM 0.0610 mL 0.3049 mL 0.6097 mL 1.5243 mL
    40 mM 0.0457 mL 0.2286 mL 0.4573 mL 1.1432 mL
    50 mM 0.0366 mL 0.1829 mL 0.3658 mL 0.9146 mL
    60 mM 0.0305 mL 0.1524 mL 0.3049 mL 0.7621 mL
    80 mM 0.0229 mL 0.1143 mL 0.2286 mL 0.5716 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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    Inquiry Information

    產(chǎn)品名稱：
    UNC0642
    目錄號(hào)：
    HY-13980
    需求量：