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  2. PROTAC Epigenetics Apoptosis Cell Cycle/DNA Damage
  3. PROTACs Histone Acetyltransferase Apoptosis Caspase PARP
  4. JQAD1

JQAD1 是 CRBN 依賴的 PROTAC，選擇性靶向 EP300 進行降解。JQAD1 抑制 EP300 表達和 H3K27ac 修飾。JQAD1 誘導細胞凋亡 (apoptosis)。JQAD1 可用于癌癥研究。

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JQAD1 Chemical Structure

JQAD1 Chemical Structure

CAS No. : 2417097-18-6

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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥1363
In-stock
5 mg ￥3000
In-stock
10 mg ￥4800
In-stock
25 mg 現(xiàn)貨 詢價
50 mg   詢價  
100 mg   詢價  

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Customer Review

  • 生物活性

  • 純度 & 產品資料

  • 參考文獻

生物活性

JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer[1].

體外研究
(In Vitro)

JQAD1 suppresses EP300 expression, suppresses the H3K27ac modification, and induces apoptosis, marked by PARP1 cleavage in control Kelly NB cells, but not in CRBN-knockout cells[1].
JQAD1 (0.5 or 1 μM; 6-96 h) treatment resulted in early time-dependent induction of a sub-G1 peak, suggestive of apoptotic cell death in Kelly and NGP cells[1].
JQAD1 (1 μM; 12-36 h) induces Kelly NB cell apoptosis[1].
JQAD1 (0.5 μM; 24 h)-treated cells exhibits upregulation of the proapoptotic BH3-only effectors BIM, BID, and PUMA together with the proapoptotic mediator BAX and its inhibitors BCL2 and MCL1[1].
JQAD1 (0.5 and 1 μM; 24 h) disrupts MYCN expression[1].
JQAD1 (0.5 μM; 24 h) causes loss of H3K27ac at chromatin[1].
JQAD1 (1.2 nM-20 μM; 5 days) has broad CRBN-dependent antineoplastic activity across cancer cell lines[1].
JQAD1 induces EP300 degradation in a time-dependent manner as early as 16 hours[1].

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

Western Blot Analysis[1]

Cell Line: MYCN-amplified NB cells
Concentration: 0.1, 0.5, 1, 3, 5, and 10 μM
Incubation Time: 24 h
Result: Demonstrated a dose-dependent decrease in EP300 expression along with a parallel loss of the H3K27ac modification. Induced selective loss of EP300 expression coincident with cleavage of PARP1, signaling the onset of apoptosis.

Western Blot Analysis[1]

Cell Line: Kelly NB cells
Concentration: 1 μM
Incubation Time: 12, 24, and 36 hours
Result: Increased the expression of cleaved caspase-3 and cleaved PARP1 in a dose-dependent manner.
體內研究
(In Vivo)

JQAD1 (40 mg/kg; i.p.; daily, for 21 d) inhibits tumor growth in NSG mice with Kelly NB cell xenografts[1].

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

Animal Model: NSG mice with Kelly NB cell xenografts[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; daily, for 21 days
Result: Suppressed tumor growth and prolonged survival.
Animal Model: CD1 mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (Pharmacokinetic Analysis)
Result: Had a half-life of 13.3 (±3.37 SD) hours in murine serum, with a Cmax of 7 μmol/L.
分子量

932.95

Formula

C48H52F4N6O9
CAS 號
性狀

固體

顏色

Light yellow to green 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 6 months
-20°C 1 month
溶解性數(shù)據
細胞實驗： 

DMSO 中的溶解度 : 100 mg/mL (107.19 mM; 超聲助溶; 吸濕的 DMSO 對產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 質量 1 mg 5 mg 10 mg
1 mM 1.0719 mL 5.3593 mL 10.7187 mL
5 mM 0.2144 mL 1.0719 mL 2.1437 mL
查看完整儲備液配制表

* 請根據產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，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
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濃度
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體積
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分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

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體積 (start)

V1

=
濃度 (final)

C2

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體積 (final)

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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

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動物的平均體重

g

每只動物的給藥體積

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由于實驗過程有損耗，建議您多配一只動物的量
計算結果
工作液所需濃度 : mg/mL
純度 & 產品資料
參考文獻

完整儲備液配制表

* 請根據產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，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0719 mL 5.3593 mL 10.7187 mL 26.7967 mL
5 mM 0.2144 mL 1.0719 mL 2.1437 mL 5.3593 mL
10 mM 0.1072 mL 0.5359 mL 1.0719 mL 2.6797 mL
15 mM 0.0715 mL 0.3573 mL 0.7146 mL 1.7864 mL
20 mM 0.0536 mL 0.2680 mL 0.5359 mL 1.3398 mL
25 mM 0.0429 mL 0.2144 mL 0.4287 mL 1.0719 mL
30 mM 0.0357 mL 0.1786 mL 0.3573 mL 0.8932 mL
40 mM 0.0268 mL 0.1340 mL 0.2680 mL 0.6699 mL
50 mM 0.0214 mL 0.1072 mL 0.2144 mL 0.5359 mL
60 mM 0.0179 mL 0.0893 mL 0.1786 mL 0.4466 mL
80 mM 0.0134 mL 0.0670 mL 0.1340 mL 0.3350 mL
100 mM 0.0107 mL 0.0536 mL 0.1072 mL 0.2680 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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產品名稱：
JQAD1
目錄號：
HY-145765
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