2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. PROTAC HSP70 Degrader-1

PROTAC HSP70 Degrader-1 (compound C4) 是一种胞质 HSP70 和 CRBN 配体，能够结合 CRBN 形成三元复合物。PROTAC HSP70 Degrader-1 介导胞质 HSP70 的泛素化和蛋白酶体降解。PROTAC HSP70 Degrader-1 对癌细胞具有细胞毒活性，可抑制肿瘤细胞增殖，与 DTHIB 联合使用时可诱导细胞凋亡。PROTAC HSP70 Degrader-1 可用于结肠癌和白血病的研究。

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PROTAC HSP70 Degrader-1

PROTAC HSP70 Degrader-1 Chemical Structure

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PROTAC HSP70 Degrader-1 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

查看所有亚型
HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC HSP70 Degrader-1 (compound C4) is a cytosolic HSP70 and CRBN ligand that can engage CRBN to form a ternary complex. PROTAC HSP70 Degrader-1 mediates ubiquitination and proteasomal degradation of cytosolic HSP70. PROTAC HSP70 Degrader-1 exhibits cytotoxic activity against cancer cells, suppressing tumor cell proliferation and inducing apoptosis in combination with DTHIB. PROTAC HSP70 Degrader-1 can be used for the research of colon cancer and leukemia[1].

体外研究
(In Vitro)

PROTAC HSP70 Degrader-1 (2-32 μM；作用 48-72 h) 可降解 RKO 细胞中的 HSP70，在 8 μM 浓度下作用 48 h 时降解率达 56%，呈现浓度和时间依赖性活性[1]。
PROTAC HSP70 Degrader-1 (8 μM；48 h) 以 8 μM 浓度处理 48 h 可使 RKO 细胞活力抑制 26%[1]。
PROTAC HSP70 Degrader-1 (8 μM; 48 h) 可在 RKO 细胞中以 8 μM 的浓度处理 48 小时后选择性降解胞质 HSP70 亚型 (HSP70α、HSP70β、HSP76)，但不会降解 BiP[1]。
PROTAC HSP70 Degrader-1 (8 μM；孵育 48 h) 与 4 μM DTHIB 联合使用可使 RKO 细胞活力抑制 78%[1]。
PROTAC HSP70 Degrader-1 (24 h) 可增加 RKO 细胞中 HSP70 的泛素化水平[1]。
PROTAC HSP70 Degrader-1 可促进 HSP70-CRBN 三元复合物的形成，而该过程会被 R17 或沙利度胺阻断[1]。
PROTAC HSP70 Degrader-1 (16 μM；72 h) 在 RKO 细胞中的 HSP70 降解活性会因CRBN敲低而受损[1]。

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

PROTAC HSP70 Degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: RKO cells
Concentration: 2-32 μM; 8 μM; 16 μM
Incubation Time: 48 h; 72 h
Result: Degraded HSP70 by 56% at 8 μM for 48 h. Exhibited concentration-dependent degradation activity across 2-32 μM for 48 h. Caused noticeable HSP70 degradation at 16 μM for 48 h, with further reduction at 72 h.

Cell Cytotoxicity Assay[1]

Cell Line: RKO cells
Concentration: 8 μM
Incubation Time: 48 h
Result: Inhibited RKO cell viability by 26% at 8 μM for 48 h.

Western Blot Analysis[1]

Cell Line: RKO cells
Concentration: 8 μM
Incubation Time: 48 h
Result: Degraded cytosolic HSP70 isoforms HSP70α, HSP70β, and HSP76 at 8 μM for 48 h but exerted minimal effect on the endoplasmic reticulum-resident BiP.

Cell Cytotoxicity Assay[1]

Cell Line: RKO cells
Concentration: 8 μM (in combination with 4 μM DTHIB)
Incubation Time: 48 h
Result: Inhibited RKO cell viability by 78% at 8 μM for 48 h when combined with 4 μM DTHIB.

Western Blot Analysis[1]

Cell Line: RKO cells
Concentration: 16 μM
Incubation Time: 72 h
Result: Lost most of its HSP70 degradation ability at 16 μM for 72 h after CRBN depletion via siRNA knockdown.
分子量

601.65

Formula

C34H31N7O4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PROTAC HSP70 Degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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 HSP70 Degrader-1HSPHeat shock proteinsHSP70βleukemiaRKO cellsBiPproteasomal degradationCRBNcolon cancerHSP76HSP70αubiquitinationInhibitorinhibitorinhibit

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