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  1. Cell Cycle/DNA Damage Anti-infection
  2. SRPK Virus Protease
  3. SRPIN340

SRPIN340 是一種 ATP 競(jìng)爭(zhēng)性的 SRPK抑制劑,能夠抑制 SRPK1 的活性,Ki 值為 0.89 μM。

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SRPIN340 Chemical Structure

SRPIN340 Chemical Structure

CAS No. : 218156-96-8

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10 mM * 1 mL in DMSO ¥770
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1 mg ¥318
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10 mg ¥1200
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Customer Review

    SRPIN340 purchased from MCE. Usage Cited in: Sci Signal. 2022 Oct 25;15(757):eabm0808.  [Abstract]

    Representative primary human type II pneumocyte culture images from samples that are pretreated with SRPIN340 (53 μM; 12 h) before they are infected with SARS-CoV-2. 24 hours later, the cells are fixed and stained for SARS-CoV-2, DNA with DAPI, and surfactant protein C (SFTPC). Scale bar, 100 μm.

    SRPIN340 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2019 Feb 26;510(1):97-103.   [Abstract]

    Bcl-2 protein expression and cleaved caspase-3 protein expression are analyzed by Western blot with or without the treatment of SRPIN340.
    • 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

    SRPIN340 is an ATP-competitive serine-arginine-rich protein kinase (SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1.

    IC50 & Target

    Ki: 0.89 μM (SRPK1)[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HL-60 IC50
    38.3 μM
    Compound: SRPIN340
    Cytotoxicity against human HL60 cells assessed as reduction in cell viability up to 200 uM after 48 hrs by MTT assay
    Cytotoxicity against human HL60 cells assessed as reduction in cell viability up to 200 uM after 48 hrs by MTT assay
    [PMID: 28407594]
    Jurkat IC50
    75.4 μM
    Compound: SRPIN340
    Cytotoxicity against human Jurkat cells assessed as reduction in cell viability up to 200 uM after 48 hrs by MTT assay
    Cytotoxicity against human Jurkat cells assessed as reduction in cell viability up to 200 uM after 48 hrs by MTT assay
    [PMID: 28407594]
    NALM-6 IC50
    70.6 μM
    Compound: SRPIN340
    Cytotoxicity against human NALM6 cells assessed as reduction in cell viability up to 200 uM after 48 hrs by MTT assay
    Cytotoxicity against human NALM6 cells assessed as reduction in cell viability up to 200 uM after 48 hrs by MTT assay
    [PMID: 28407594]
    體外研究
    (In Vitro)

    SRPIN340 是一種富含絲氨酸精氨酸的蛋白激酶 (SRPK) 抑制劑,對(duì) SRPK1 的 Ki 為 0.89 μM。SRPIN340 也抑制 SRPK2,但對(duì)其他 SRPK (例如 Clk1 和 Clk4) 沒(méi)有顯著抑制作用。SRPIN340 促進(jìn) SRp75 的降解,這是 HIV 表達(dá)所必需的。SRPIN340 抑制 Sindbis 病毒 (IC50,60 μM) 以及嚴(yán)重急性呼吸系統(tǒng)綜合癥病毒的傳播[1]。SRPIN340 對(duì) AML HL60、ALL-T Molt4 和 Jurkat 等白血病細(xì)胞系具有抑制作用,IC50 分別為 44.7 μM、92.2 μM 和 82.3 μM[2]。

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

    分子量

    349.35

    Formula

    C18H18F3N3O

    CAS 號(hào)
    性狀

    固體

    顏色

    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 : ≥ 42 mg/mL (120.22 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.8625 mL 14.3123 mL 28.6246 mL
    5 mM 0.5725 mL 2.8625 mL 5.7249 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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.16 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(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

    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: 99.97%

    參考文獻(xiàn)
    Cell Assay
    [2]

    Leukemic cells (5 × 104 cells/well) and isolated PBMCs (8 × 104 cells/well) are seeded in 96-well plates. Each well contained 100 μL of complete RPMI medium and 100 μL of SRPIN340 solution at different concentrations. The compound is diluted in RPMI medium with 10% fetal bovine serum and 0.4% DMSO (v/v). After 48 h of culture, MTT (5 mg/mL) is added to the wells (3 h, 37°C). The plates are centrifuged at room temperature for 30 min 500 ×g, followed by the removal of the MTT solution and the addition of 100 μL/well of DMSO to solubilize the formazan. Absorbance is measured at 540 nm in a microplate reader. Each experimental procedure is performed in triplicate[2].

    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 2.8625 mL 14.3123 mL 28.6246 mL 71.5615 mL
    5 mM 0.5725 mL 2.8625 mL 5.7249 mL 14.3123 mL
    10 mM 0.2862 mL 1.4312 mL 2.8625 mL 7.1561 mL
    15 mM 0.1908 mL 0.9542 mL 1.9083 mL 4.7708 mL
    20 mM 0.1431 mL 0.7156 mL 1.4312 mL 3.5781 mL
    25 mM 0.1145 mL 0.5725 mL 1.1450 mL 2.8625 mL
    30 mM 0.0954 mL 0.4771 mL 0.9542 mL 2.3854 mL
    40 mM 0.0716 mL 0.3578 mL 0.7156 mL 1.7890 mL
    50 mM 0.0572 mL 0.2862 mL 0.5725 mL 1.4312 mL
    60 mM 0.0477 mL 0.2385 mL 0.4771 mL 1.1927 mL
    80 mM 0.0358 mL 0.1789 mL 0.3578 mL 0.8945 mL
    100 mM 0.0286 mL 0.1431 mL 0.2862 mL 0.7156 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:
    SRPIN340
    目錄號(hào):
    HY-13949
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