2. Metabolic Enzyme/Protease
  3. Hexokinase
  4. PROTAC HK2 Degrader-1

PROTAC HK2 Degrader-1 

目录号: HY-155008 纯度: 98.66%
COA 产品使用指南

摩尔计算器

PROTAC HK2 Degrader-1 是靶向 Hexokinase 2 (HK2) 的 PROTAC。PROTAC HK2 Degrader-1 由 Hexokinase 2 (HK2) 抑制剂 Lonidamine (HY-B0486)，CRBN 配体 Thalidomide (HY-14658) 组成。PROTAC HK2 Degrader-1通过泛素-蛋白酶体系统形成一个三元复合体降解 Hexokinase 2 (HK2) 蛋白诱导线粒体损伤，引发细胞焦亡 (pyroptosis)。PROTAC HK2 Degrader-1 能有效抑制乳腺肿瘤的生长，并减少 Cisplatin (HY-17394) 的结肠副作用。可用于乳腺癌的研究。

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PROTAC HK2 Degrader-1 Chemical Structure

PROTAC HK2 Degrader-1 Chemical Structure

CAS No. : 3033812-84-6

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规格 价格 是否有货 数量
1 mg ￥1260
In-stock
5 mg ￥2770
In-stock
10 mg ￥4430
In-stock
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Customer Review

PROTAC HK2 Degrader-1 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research[1].

IC50 & Target

DC50: 2.56 μM (Hexokinase 2, HK2 in 4T1); 0.79 μM ((Hexokinase 2, HK2 in MDA-MB-231)
体外研究
(In Vitro)

PROTAC HK2 Degrader-1 抑制 786-O，4T1，PANC-1，HGC-27，MCF-1 细胞增殖的 IC50 分别为34.07 μM，5.08 μM，31.53 μM，6.11 μM，21.65 μM[1]。
PROTAC HK2 Degrader-1 对 HK2 的 DC50 为2.56 μM (4T1) 和 0.79 μM (MDA-MB-231)[1]。
PROTAC HK2 Degrader-1 (0.01-200 μM, 36 h) 选择性地抑制乳腺癌细胞增殖，并通过泛素介导的蛋白酶体途径，以时间和浓度依赖的方式刺激HK2蛋白的降解[1]。
PROTAC HK2 Degrader-1 (10 μM for 4T1, 0.5 μM for MDA-MB-231, 24 h) 通过泛素-蛋白酶体系统形成一个三元复合体降解HK2蛋白[1]。
这一句可作为机制，放到产品总描述中。 PROTAC HK2 Degrader-1 (20 μM, 36 h) 降解HK2导致线粒体损伤后释放细胞色素C激活caspase-3，裂解GSDME引发热昏迷从而细胞释放危险信号，如ATP、HMGB1、CRT等，最后导致诱发细胞免疫死亡[1]。
PROTAC HK2 Degrader-1 (20 μM, 36 h) 能诱导 PD-L1 蛋白从细胞膜内化到细胞质，并减少 PD-L1 蛋白的总量[1]。

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

PROTAC HK2 Degrader-1 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: 4T1, MDA-MB-231, PUMC-HUVEC-T1
Concentration: 20 μM
Incubation Time: 72 h (MTT), 48 h (CCK-8)
Result: Showed the greatest impact on 4T1 and HGC-27 cells, with IC50 dosages of 5.08 and 6.11 μM.
Selectively suppressed breast cancer cell proliferation and stimulates HK2 protein degradation.
Prevented 4T1 cells to form a colony and had little influence on HUVECT-1.

Western Blot Analysis[1]

Cell Line: 4T1, MDAMB-231
Concentration: 20 μM; 0.01, 0.05, 0.1, 0.5, 1.0, 2.0, 5.0, 10, 20, 50, 100, 150, 200 μM; 10 μM; 0.5 μM.
Incubation Time: 36 h; 24 h
Result: Degraded 71.06% of HK2 at 20 μM in 4T1 and MDAMB-231 cells.
DC50=2.56 μM (4T1) and 0.79 μM (MDA-MB-231), respectivley.
Promoted the degradation of HK2 protein within 12 h, with the greatest degradation impact at 36 h in 4T1 cells and MDA-MB-231 cells.
Degradation capacity was reduced, because pretreatment with Tha and LND occupy the protein pocket and disrupt the formation of the ternary complex of HK2, CRBN and C-02.
Increased the expression of VDAC and Bax and decreased the level of Bcl-2 protein.
had lower levels of full-length caspase-3 and higher levels of cleaved caspase-3.
Cleaved GSDME through cleaved caspase-3, increasing the N-terminus of GSDME protein and thus triggering pyroptosis in 4T1 cells.

Immunofluorescence[1]

Cell Line: 4T1 and MDA-MB-231
Concentration: 20 μM
Incubation Time: 36 h
Result: Caused the degradation of HK2 protein in a concentration dependent manner.
Significantly reduced the visual yellow fluorescence of HK2 protein.
体内研究
(In Vivo)

PROTAC HK2 Degrader-1 (50 mg/kg, Intraperitoneal injection, bid, for nine times, six-weekold female BALB/c mice) 需要提及造模动物是什么~）抑制4T1肿瘤模型的肿瘤生长[1]。
PROTAC HK2 Degrader-1 (50 mg/kg, Intraperitoneal injection, bid, for nine times, six-weekold female BALB/c mice) 能诱导GSDME依赖性的热化反应，实现肿瘤免疫反应，有效抑制乳腺肿瘤的生长[1]。
PROTAC HK2 Degrader-1 (Cisplatin (HY-17394) 10mg/kg, i.v., C-02 50mg/kg, i.p., 25 days, six-weekold female BALB/c mice) 可以使顺铂增敏，同时减少顺铂的结肠副作用，具有潜在的临床价值[1]。

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

Animal Model: xenograft models , into six-weekold female BALB/c mice[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection, bid, for nine times.
Result: Reduced proliferation and damaged nuclei in mouse models.
Increased the levels of Cytokines IL-1β, IFN-γ, and TNF-α significantly and decreased the level of TGF-β and IL-10.
Elevated levels of cleaved-Casp-3 and GSDME-N in tumor tissues of mouse.
Animal Model: breast tumor model in mice by injecting 4T1 cells subcutaneously into six-weekold female BALB/c mice[1]
Dosage: Cisplatin (HY-17394) 10mg/kg, 50mg/kg
Administration: Cisplatin (HY-17394) (10mg/kg, i.v.), 50mg/kg, i.p., 25 days
Result: Inhibited tumor growth and tumor volume.
Decreased HK2 protein level, while co- treated with Cisplatin (HY-17394).
Could alleviate Cisplatin (HY-17394) aggravated colon damage.
分子量

647.51

Formula

C32H28Cl2N6O5
CAS 号
性状

固体

颜色

Light yellow to 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
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (154.44 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 1.5444 mL 7.7219 mL 15.4438 mL
5 mM 0.3089 mL 1.5444 mL 3.0888 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

PROTAC HK2 Degrader-1 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 1.5444 mL 7.7219 mL 15.4438 mL 38.6094 mL
5 mM 0.3089 mL 1.5444 mL 3.0888 mL 7.7219 mL
10 mM 0.1544 mL 0.7722 mL 1.5444 mL 3.8609 mL
15 mM 0.1030 mL 0.5148 mL 1.0296 mL 2.5740 mL
20 mM 0.0772 mL 0.3861 mL 0.7722 mL 1.9305 mL
25 mM 0.0618 mL 0.3089 mL 0.6178 mL 1.5444 mL
30 mM 0.0515 mL 0.2574 mL 0.5148 mL 1.2870 mL
40 mM 0.0386 mL 0.1930 mL 0.3861 mL 0.9652 mL
50 mM 0.0309 mL 0.1544 mL 0.3089 mL 0.7722 mL
60 mM 0.0257 mL 0.1287 mL 0.2574 mL 0.6435 mL
80 mM 0.0193 mL 0.0965 mL 0.1930 mL 0.4826 mL
100 mM 0.0154 mL 0.0772 mL 0.1544 mL 0.3861 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:

PROTAC HK2 Degrader-13033812-84-6HexokinaseHexokinase 2HK2lonidamineLNDthalidomideTha4T1MDA-MB-231MCF-7PROTACbreast cancer.Inhibitorinhibitorinhibit

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