TPI-1
(Synonyms: Tyrosine Phosphatase Inhibitor 1) 目录号 : GC18239
TPI-1（酪氨酸磷酸酶抑制剂1）是一种SHP-1抑制剂（IC50 = 40nM），可用于研究黑色素瘤。
Cas No.:79756-69-7
Sample solution is provided at 25 µL, 10mM.
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TPI-1 (tyrosine phosphatase inhibitor 1) is a SHP-1 inhibitor (IC50 = 40nM) and can be used to study melanomas[1].
TPI-1 (0.01μg/ml, 0.1μg/ml, 1μg/ml, and 3μg/ml; 10min) selectively increases SHP-1 phospho-substrates in Jurkat T cells at low nM (0.01-0.1μg/ml)[1]. TPI-1 (5μM, 30min) increased macrophage phagocytosis through activating STAT3 and STAT6 signaling pathways[2]. TPI-1 (5μM, 2h) could reverse the decreased phosphorylation of both ERK and STAT3 and restore NK cell cytotoxicity under hypoxia in the NK cell line KHYG-1[3].
TPI-1 (1 or 3mg/kg/day, 4 days, s.c.) increases spleen pLck-pY394 and IFNγ+ cells in C57BL/6J mice[1]. TPI-1 (3mg/kg/d, 5 days/week, terminated by the third week, p.o.) inhibited tumor growth, inducing approximately 83% growth inhibition (p < 0.002) compared to the control in the B16 melanoma mouse model[1].
References:
[1] Kundu S, Fan K, Cao M, et al. Novel SHP-1 inhibitors tyrosine phosphatase inhibitor-1 and analogs with preclinical anti-tumor activities as tolerated oral agents. The Journal of Immunology. 2010 Jun 1;184(11):6529-36.
[2] Shen Q, Zhao L, Pan L, et al. Soluble SIRP-alpha promotes murine acute lung injury through suppressing macrophage phagocytosis. Frontiers in Immunology. 2022 May 12;13:865579.
[3] Teng R, Wang Y, Lv N, et al. Hypoxia Impairs NK Cell Cytotoxicity through SHP‐1‐Mediated Attenuation of STAT3 and ERK Signaling Pathways. Journal of Immunology Research. 2020;2020(1):4598476.
TPI-1（酪氨酸磷酸酶抑制剂1）是一种SHP-1抑制剂（IC50 = 40nM），可用于研究黑色素瘤[1]。
TPI-1（0.01μg/ml、0.1μg/ml、1μg/ml和3μg/ml，10分钟）在低nM（0.01-0.1μg/ml）下选择性增加Jurkat T细胞中的SHP-1磷酸化底物[1]。TPI-1（5μM，30分钟）通过激活STAT3和STAT6信号通路增加巨噬细胞吞噬作用[2]。TPI-1（5μM，2小时）可以逆转ERK和STAT3磷酸化的降低，并恢复NK细胞系KHYG-1缺氧下的NK细胞毒性[3]。
TPI-1（1或3mg/kg/天，4天，皮下注射）可增加C57BL/6J小鼠脾脏pLck-pY394和IFNγ+细胞[1]。在B16黑色素瘤小鼠模型中，与对照组相比，TPI-1（3mg/kg/天，5天/周，三周，口服）可抑制肿瘤生长，其生长抑制率约为83%（p < 0.002）[1]。
| Cell experiment [1]: | |
Cell lines | Jurkat human T cell line |
Preparation Method | Jurkat cells in culture medium (3×106 cells/ml) were untreated or treated with TPI-1 at various doses (0.01μg/ml, 0.1μg/ml, 1μg/ml, and 3μg/ml) for 10min. After brief centrifuging in a microfuge (4,000rpm, 2min), the cell pellet was lysed on ice for 30min in 100µl of cold lysis buffer (1% NP40, 50mM Tris, pH 7.4, 150mM NaCl, 20mM NaF, 0.2mM Na3VO4 and 1mM Na3MO4) containing a cocktail of proteinase inhibitors. The lysates were cleared by centrifuging (14,000rpm, 10min) in a microfuge at 4°C to remove insoluble parts, mixed with equal volume of 2×SDS-PAGE sample buffer, boiled for 5min and analyzed by SDS-PAGE/Western blotting. |
Reaction Conditions | 0.01μg/ml, 0.1μg/ml, 1μg/ml, and 3μg/ml; 10min |
Applications | TPI-1 selectively increases SHP-1 phospho-substrates in Jurkat T cells at low nM (0.01-0.1μg/ml). |
| Animal experiment [1]: | |
Animal models | B16 Melanoma mouse model |
Preparation Method | C57BL/B6 mice (n = 5) were inoculated (s.c.) at the flanks with B16 murine melanoma cells. Four days post-inoculation, the mice were treated with oral TPI-1 (3mg/kg/d, 5 days/week). Tumor volumes were measured during the study period and calculated using the formula for a prolate spheroid (V= 4/3 πa2b). |
Dosage form | 3mg/kg/d, 5 days/week, terminated by the third week, p.o. |
Applications | TPI-1 inhibited tumor growth, inducing approximately 83% growth inhibition (p < 0.002) compared to the control in the B16 melanoma mouse model. |
References: | |
| Cas No. | 79756-69-7 | SDF | |
| 别名 | Tyrosine Phosphatase Inhibitor 1 | ||
| 化学名 | 2-(2,5-dichlorophenyl)-2,5-cyclohexadiene-1,4-dione | ||
| Canonical SMILES | ClC1=C(C(C(C=C2)=O)=CC2=O)C=C(Cl)C=C1 | ||
| 分子式 | C12H6Cl2O2 | 分子量 | 253.1 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.951 mL | 19.755 mL | 39.5101 mL |
| 5 mM | 0.7902 mL | 3.951 mL | 7.902 mL |
| 10 mM | 0.3951 mL | 1.9755 mL | 3.951 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Quality Control & SDS
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- Purity: >98.00%
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