1. PROTAC Metabolic Enzyme/Protease Stem Cell/Wnt Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Immunology/Inflammation
  2. PROTACs Phosphatase JAK IFNAR MHC
  3. TP1L

TP1L 是一种强效、选择性的 T 细胞蛋白酪氨酸磷酸酶 (TC-PTP) PROTAC 降解剂,DC50 值为 35.8 nM。TP1L 能提高 TC-PTP 底物的磷酸化水平,包括 pSTAT1pJAK1。TP1L 选择性地增强 IFN-γ 信号传导并增加 MHC-I 的表达。TP1L 通过增加 LCK 的磷酸化激活 TCR 信号传导。TP1L 通过激活 CAR-T 细胞增强 CAR-T 细胞介导的肿瘤杀伤效能。TP1L 可用于癌症研究。(粉色:TC-PTP 配体:(HY-138964),蓝色:E3 连接酶 CRBN 配体 (HY-A0003),黑色:连接子:(HY-140002)。

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TP1L

TP1L Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TP1L is a potent and selective T-cell protein tyrosine phosphatase (TC-PTP) PROTAC degrader, with a DC50 value of 35.8 nM. TP1L elevates the phosphorylation level of TC-PTP substrates including pSTAT1 and pJAK1. TP1L selectively enhances IFN-γ signaling and increases MHC-I expression. TP1L activates TCR signaling through increases phosphorylation of LCK. TP1L enhances CAR-T cell mediated tumor killing efficacy through activation of the CAR-T cells. TP1L can be used for the study of cancer. (Pink: TC-PTP ligand: (HY-138964), Blue: E3 ligase CRBN Ligand (HY-A0003), Black: Linker: (HY-140002))[1].

体外研究
(In Vitro)

TP1L (0.5-4000 nM, 3-24 h) 在 HEK293 细胞中通过泛素化-蛋白酶体途径选择性地降解 TC-PTP (DC50 = 35.8 nM)[1]
TP1L (<10 μM) 即使在浓度高达 10 μM 时,对其他蛋白酪氨酸磷酸酶 (PTPs) 也没有显著的抑制作用。 TP1L (0.5-4000 nM, 3-24 h) 在 HEK293 细胞中选择性地增强 IFN-γ 信号传导并促进抗原呈递[1]
TP1L (62.5-1000 nM, 16 h) 在 Jurkat T 细胞中提高 pLCK 水平,并在 KB 肿瘤/CAR-T 细胞共培养系统中增强 CAR-T 细胞的杀伤效率[1]

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

Western Blot Analysis[1]

Cell Line: HEK293 cells and Jurkat T-cells
Concentration: 0.5, 3.9, 7.8, 15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000, 4000 nM
Incubation Time: 3, 6, 16, 24 h
Result: Degradated TC-PTP with a DC50 of 35.8 nM in HEK293 cells after 16 hours of treatment.
Showed no signicantly altered on the level of PTP1Bat up to 4 mM concentration.
Degradated TC-PTP completly within 6 hours.
Did not decrease during the entire period of TP1L treatment.
Enhanced the levels of pJAK1 and pSTAT1.
Did not affected the phosphorylation level of JAK2, which is a substrate of PTP1B.
Degraded TC-PTP and promoted phosphorylation of LCK in Jurkat T-cells.
分子量

1255.34

Formula

C64H81F2N8O14P

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
  • 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 *
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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.

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产品名称:
TP1L
目录号:
HY-160151
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