2. Stem Cell/Wnt PROTAC
  3. YAP PROTACs
  4. KG-FP-003

KG-FP-003 是一种高效、选择性的且持久的 TEAD PROTAC 类降解剂 (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM)。KG-FP-003 能促进 TEAD 的泛素化和降解。KG-FP-003 对间皮瘤和卵巢癌具有抗癌活性。
(粉色: Ligands for Target Protein for PROTAC 和 TEAD 配体 (HY-186118)；蓝色: Ligands for E3 Ligase 和 Cereblon E3 连接酶配体；黑色: 连接子)。

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KG-FP-003

KG-FP-003 Chemical Structure

CAS No. : 3066008-42-9

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Customer Review

KG-FP-003 相关抗体

Top Publications Citing Use of Products

查看 YAP 亚型特异性产品:

查看所有亚型
YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KG-FP-003 is a highly potent, selective, and durable TEAD PROTAC degrader (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM). KG-FP-003 promotes ubiquitination and degradation of TEAD. KG-FP-003 exhibits anticancer activity against mesothelioma and ovarian cancer[1]. (Pink: Ligands for Target Protein for PROTAC and TEAD ligand (HY-186118); Blue: Ligands for E3 Ligase and Cereblon E3 ligase ligand; Black: linker).

IC50 & Target[1]

Cereblon

 

TEAD1

6 nM (DC50)

TEAD2

68 nM (DC50)

TEAD3

12 nM (DC50)

TEAD4

7 nM (DC50)

体外研究
(In Vitro)

KG-FP-003 以 591 ± 21 nM 的 IC50 结合重组 CRBN-DDB1ΔBPB 蛋白[1]。
KG-FP-003 (以 10 μM 的浓度进行 3 倍梯度稀释; 2 h) 在过表达 NanoLuc-CRBN 的 HEK293T 细胞中与 CRBN 结合，在细胞结合实验中的 IC50 为 962 ± 86 nM[1]。
KG-FP-003 (6 h) 可在处理 6 h 后强效且选择性地降解 HiBiT 标记 HEK293T 细胞中的全部四种 TEAD 亚型 (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM)[1]。
KG-FP-003 (72 h) 可强效抑制 NCI-H226 间皮瘤细胞的增殖，处理 72 h 后的 IC50 为 27 ± 7 nM[1]。

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

KG-FP-003 相关抗体:

Real Time qPCR[1]

Cell Line: MSTO-211H mesothelioma cells
Concentration: 300 nM
Incubation Time: Unclear
Result: Induced dramatic upregulation of the pro-apoptotic gene BMF and downregulation of the TEAD target gene CTGF.

Cell Cycle Analysis[1]

Cell Line: MSTO-211H mesothelioma cells
Concentration: 100-1000 nM
Incubation Time: 24 h
Result: Increased the percentage of cells in G1 phase from 54.3% to 62.1% at 100 nM, and to 65.2% at 1000 nM, indicating G1 phase cell cycle arrest.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax T1/2 MRT0-inf AUC0-last AUC0-inf Bioavailability
Mice[1] 2 mg/kg i.v. 0 h 4431 ng/mL 3.57 h 1.4 h 1043 ng·h/mL 1056 ng·h/mL /
Mice[1] 5 mg/kg i.p. 0.42 h 2007 ng/mL 5.42 h 3.13 h 2560 ng·h/mL 2612 ng·h/mL 99 %
体内研究
(In Vivo)

KG-FP-003 (腹腔注射；每日 1 次；连续 21 天；剂量 3-30 mg/kg) 在 NF2 缺陷型 MSTO-211H 间皮瘤异种移植模型中表现出显著的剂量依赖性抗肿瘤活性[1]。
KG-FP-003 (腹腔注射；每日 1 次；连续 21 天，剂量 10-30 mg/kg) 在 10 mg/kg 和 30 mg/kg 剂量下可显著诱导 ES2 卵巢癌异种移植瘤消退[1]。

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

Animal Model: BALB/c nude (6-week-old)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: i.p.; once daily; 21 days
Result: Induced pronounced degradation of TEAD1 protein and significant tumor growth inhibition compared to vehicle controls.
Achieved a tumor growth inhibition (TGI) rate of 118% at 10 mg/kg.
Achieved a TGI rate of 129% at 30 mg/kg.
Maintained stable body weights in all treated mice throughout the 21-day treatment period.
分子量

1049.64

Formula

C58H67ClF2N6O8
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

KG-FP-003 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)

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

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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:

KG-FP-0033066008-42-9YAPPROTACsYes-associated proteinxenograft modelsHippo signalingCRBNTEAD4malignant pleural mesotheliomaglioblastoma multiformeBALB/c nude miceTEAD2TEAD3ubiquitin-proteasome systemInhibitorinhibitorinhibit

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产品名称：
KG-FP-003
目录号：
HY-186117
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