2. PROTAC Stem Cell/Wnt
  3. PROTACs YAP
  4. HC278

HC278 是一种选择性的 TEAD1/TEAD3 PROTAC 降解剂。HC278 可通过与 CRBN/DDB1 形成稳定的三元复合物，诱导蛋白酶体依赖性降解。HC278 可用于间皮瘤的研究。

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HC278

HC278 Chemical Structure

CAS No. : 3096503-40-8

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HC278 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 YAP 亚型特异性产品:

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HC278 is a selective TEAD1/TEAD3 PROTAC degrader. HC278 induces proteasome-dependent degradation by forming a stable ternary complex with CRBN/DDB1. HC278 is applicable to the research of mesothelioma[1].

体外研究
(In Vitro)

HC278 (50-500 nM; 2-18 h) 是一种依赖蛋白酶体和 CRBN 的 PROTAC，可在表达表位标记 TEAD1-4 的 HEK293 稳定细胞中强效且选择性地降解 TEAD1 和 TEAD3；在 50 nM 浓度下即可观察到显著的降解效果，而在 500 nM 浓度下对 TEAD2 的影响极小，对 TEAD4 仅具有弱活性[1]。
HC278 (100-200 nM; 2 周) 可在 200 nM 浓度下特异性抑制 YAP 依赖性 NCI-H226 间皮瘤细胞的集落形成能力，而对作为对照的 NCI-H28 间皮瘤细胞无影响[1]。
HC278 (500 nM; 24 h) 可抑制 NCI-H226 间皮瘤细胞中的 TEAD/YAP 转录活性，在 500 nM 作用 24 h 时显著下调 YAP 特征基因及包括 CTGF、CYR61 和 ANKRD1 在内的特异性靶基因[1]。
HC278 (500 nM-1 μM; 24 h) 可在 500 nM、1 μM 作用 24 h 时下调 MDA-MB-231 细胞中 YAP 靶基因 (CTGF、CYR61、ANKRD1) 的表达[1]。

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

HC278 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK293 stable cells expressing epitope-tagged TEAD1-4 (FLAG-TEAD1, MYC-TEAD2, V5-TEAD3, HA-TEAD4)
Concentration: 50 nM; 500 nM
Incubation Time: 2 h, 4 h, 6 h, 8 h, 10 h, 12 h, 14 h, 16 h, 18 h
Result: Degraded TEAD1 and TEAD3 by more than 50% at 50 nM.
Had little effect on TEAD2, and only a weak degrading effect on TEAD4 at 500 nM.
Detected TEAD1/3 degradation as early as 2 h after treatment, with degradation increasing over time.
Completely blocked TEAD degradation when co-treated with 1 μM MG132.
Inhibited TEAD degradation activity when co-treated with 500 nM Ex.
29.
Showed much weaker degradative effect for negative control HC278-Neg1, and failed to induce TEAD degradation for negative control HC278-Neg2.

Cell Proliferation Assay[1]

Cell Line: NCI-H226 mesothelioma cells, NCI-H28 control mesothelioma cells
Concentration: 100 nM; 200 nM
Incubation Time: two weeks
Result: Significantly inhibited the colony-forming ability of NCI-H226 cells (YAP-dependent, NF2-deleted) at 200 nM, with little effect at 100 nM.
Had no apparent effect on the colony-forming ability of NCI-H28 cells (control, no Hippo pathway mutations) even at 200 nM.

Real Time qPCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 500 nM; 1 μM
Incubation Time: 24 h
Result: Significantly downregulated the mRNA levels of YAP target genes CTGF, CYR61, and ANKRD1 compared to DMSO-treated cells.
分子量

776.80

Formula

C43H39F3N6O5
CAS 号
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

HC278 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

HC2783096503-40-8HC 278HC-278PROTACsYAPYes-associated proteinTEAD1mesotheliomaNCI-H28DDB1CRBNTEAD3NCI-H226HEK293 stable cellsMDA-MB-231Inhibitorinhibitorinhibit

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