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  2. Epigenetics Apoptosis
  3. DNA Methyltransferase Apoptosis
  4. SGI-1027

SGI-1027 是 DNA 甲基轉(zhuǎn)移酶 (DNMT) 抑制劑，對以 poly(dI-dC) 為底物的 DNMT3B，DNMT3A 和 DNMT1 的 IC50 值分別為 7.5 μM，8 μM 和 12.5 μM。

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SGI-1027 Chemical Structure

SGI-1027 Chemical Structure

CAS No. : 1020149-73-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥690
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1 mg ￥272
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5 mg ￥680
In-stock
10 mg ￥1083
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50 mg ￥3448
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200 mg   詢價(jià)  

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查看 DNA Methyltransferase 亞型特異性產(chǎn)品:

  • 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

SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.

IC50 & Target[1]

DNMT3B

7.5 μM (IC50)

DNMT3A

8 μM (IC50)

DNMT1

12.5 μM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 EC50
> 10 μM
Compound: SGI1027
Antiproliferative activity against human HCT116 cells after 2 to 4 days by ATPlite 1step luminescence assay
Antiproliferative activity against human HCT116 cells after 2 to 4 days by ATPlite 1step luminescence assay
[PMID: 26220519]
HCT-116 IC50
3.2 μM
Compound: SGI-1027
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue assay
[PMID: 34333394]
K562 IC50
1.16 μM
Compound: SGI-1027
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
[PMID: 28419930]
KARPAS-299 EC50
1.8 μM
Compound: SGI1027
Antiproliferative activity against human KARPAS299 cells after 2 to 4 days by ATPlite 1step luminescence assay
Antiproliferative activity against human KARPAS299 cells after 2 to 4 days by ATPlite 1step luminescence assay
[PMID: 26220519]
KG-1 EC50
4.4 μM
Compound: SGI1027
Antiproliferative activity against human KG1 cells after 2 to 4 days by ATPlite 1step luminescence assay
Antiproliferative activity against human KG1 cells after 2 to 4 days by ATPlite 1step luminescence assay
[PMID: 26220519]
MDA-MB-231 IC50
4.8 μM
Compound: 1, SGI-1027
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by trypan blue exclusion assay
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by trypan blue exclusion assay
[PMID: 24387159]
PBMC IC50
23.8 μM
Compound: 1, SGI-1027
Cytotoxicity against human PBMC after 48 hrs by trypan blue exclusion assay
Cytotoxicity against human PBMC after 48 hrs by trypan blue exclusion assay
[PMID: 24387159]
PC-3 IC50
6.5 μM
Compound: 1, SGI-1027
Cytotoxicity against human PC3 cells after 48 hrs by trypan blue exclusion assay
Cytotoxicity against human PC3 cells after 48 hrs by trypan blue exclusion assay
[PMID: 24387159]
Raji IC50
9.1 μM
Compound: 1, SGI-1027
Cytotoxicity against human Raji cells after 48 hrs by trypan blue exclusion assay
Cytotoxicity against human Raji cells after 48 hrs by trypan blue exclusion assay
[PMID: 24387159]
Sf9 IC50
6 μM
Compound: 7, SGI1027
Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil
Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil
[PMID: 25406944]
Sf9 IC50
7.5 μM
Compound: 7, SGI1027
Inhibition of His6-tagged human recombinant DNMT3b expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scinti
Inhibition of His6-tagged human recombinant DNMT3b expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scinti
[PMID: 25406944]
Sf9 IC50
8 μM
Compound: 7, SGI1027
Inhibition of His6-tagged human recombinant DNMT3a expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scinti
Inhibition of His6-tagged human recombinant DNMT3a expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scinti
[PMID: 25406944]
U-937 IC50
1.56 μM
Compound: SGI-1027
Antiproliferative activity against human U937 cells after 72 hrs by MTT assay
Antiproliferative activity against human U937 cells after 72 hrs by MTT assay
[PMID: 28419930]
U-937 IC50
1.7 μM
Compound: 1, SGI-1027
Cytotoxicity against human U937 cells after 48 hrs by trypan blue exclusion assay
Cytotoxicity against human U937 cells after 48 hrs by trypan blue exclusion assay
[PMID: 24387159]
體外研究
(In Vitro)

SGI-1027 是一種 DNMT 抑制劑，以聚 (dI-dC) 為底物時(shí)，對 DNMT3B、DNMT3A 和 DNMT1 的 IC50 分別為 7.5 μM、8 μM 和 12.5 μM。SGI-1027 對 DNMT1 (半甲基化 DNA) 的 IC50 為 6 μM。SGI-1027 (1、2.5 或 5 μM) 在幾種人類癌細(xì)胞系中引起 DNMT1 的選擇性降解，但對大鼠肝癌細(xì)胞幾乎沒有或沒有細(xì)胞毒性作用，并且不會誘導(dǎo)大鼠肝癌細(xì)胞凋亡[1]。SGI-1027 對 hDNMT3A 的 EC50 為 0.9 μM，并對 KG-1 細(xì)胞產(chǎn)生細(xì)胞毒性，EC50 為 4.4 μM[2]。

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

461.52

Formula

C27H23N7O
CAS 號
性狀

固體

顏色

Light yellow to yellow

運(yùn)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(shí)驗(yàn)： 

DMSO 中的溶解度 : 27 mg/mL (58.50 mM; 超聲加熱助溶; 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)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.1668 mL 10.8338 mL 21.6675 mL
5 mM 0.4334 mL 2.1668 mL 4.3335 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(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?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

動物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)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(shí)驗(yàn)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(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 (5.42 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 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 (5.42 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 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(jì)算器
請輸入動物實(shí)驗(yàn)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

只
由于實(shí)驗(yàn)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(jì)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(shí)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(shí)驗(yàn)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)
Kinase Assay
[1]

To determine the nature of inhibition of DNMTase activity by SGI-1027, DNMT1 enzyme activity is measured in presence of a fixed concentration of SGI-1027 (0, 2.5, 5, and 10 μM) while one of the two (Ado-Met or DNA) is varied in a particular reaction mixture. At a fixed concentration of DNA (500 ng) varying concentrations of Ado-Met used are from 25-500 nM, respectively. Similarly, final DNA concentrations are varied from (25-500 ng) at 75 nM Ado-Met[1].

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

Rat hepatoma H4IIE cells are grown in DMEM supplemented with fetal bovine serum (10%) and calf serum (10%). Cells are seeded into 96-well plates and after 48 h exposed to SGI-1027 at concentrations ranging from 0 to 300 μM. The solubility is determined by Nephalometry techniques immediately after dosing and before harvesting the cells at 24 h. Following the exposure period, the cells or their supernatant (culture medium) are analyzed for changes in cell proliferation (propidium iodide), membrane leakage (α-GST), mitochondrial function [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and cellular ATP], oxidative stress (intracellular GSH and 8-isoprostane), and apoptosis (caspase-3). The half-maximal toxic concentration (TC50) is determined from the dose-response curves[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?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 2.1668 mL 10.8338 mL 21.6675 mL 54.1688 mL
5 mM 0.4334 mL 2.1668 mL 4.3335 mL 10.8338 mL
10 mM 0.2167 mL 1.0834 mL 2.1668 mL 5.4169 mL
15 mM 0.1445 mL 0.7223 mL 1.4445 mL 3.6113 mL
20 mM 0.1083 mL 0.5417 mL 1.0834 mL 2.7084 mL
25 mM 0.0867 mL 0.4334 mL 0.8667 mL 2.1668 mL
30 mM 0.0722 mL 0.3611 mL 0.7223 mL 1.8056 mL
40 mM 0.0542 mL 0.2708 mL 0.5417 mL 1.3542 mL
50 mM 0.0433 mL 0.2167 mL 0.4334 mL 1.0834 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：
SGI-1027
目錄號：
HY-13962
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