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

JQAD1 是 CRBN 依赖的 PROTAC，选择性靶向 EP300 进行降解。JQAD1 抑制 EP300 表达和 H3K27ac 修饰。JQAD1 诱导细胞凋亡 (apoptosis)。JQAD1 可用于癌症研究。

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JQAD1 Chemical Structure

JQAD1 Chemical Structure

CAS No. : 2417097-18-6

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规格 价格 是否有货 数量
1 mg ￥1363
In-stock
5 mg ￥3000
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10 mg ￥4800
In-stock
25 mg ￥9500
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Customer Review

JQAD1 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 PARP 亚型特异性产品:

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

体外研究
(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.

JQAD1 相关抗体:

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.
体内研究
(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 号
性状

固体

颜色

Light yellow to green yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (107.19 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

JQAD1 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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.

Keywords:

JQAD12417097-18-6JQAD 1JQAD-1PROTACsHistone AcetyltransferaseApoptosisCaspasePARPHATsHATpoly ADP ribose polymeraseCRBNH3K27acKelly NBNGPMYCNNSG miceInhibitorinhibitorinhibit

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