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TPI-1 是一种 SHP-1的抑制剂,其 IC50=40 nM。

TPI-1 是一种 SHP-1的抑制剂,其 IC50=40 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 397 | In stock | |
| 2 mg | ¥ 587 | In stock | |
| 5 mg | ¥ 997 | In stock | |
| 10 mg | ¥ 1,730 | In stock | |
| 25 mg | ¥ 2,970 | In stock | |
| 50 mg | ¥ 4,380 | In stock | |
| 100 mg | ¥ 6,230 | In stock | |
| 500 mg | ¥ 12,700 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 995 | In stock |
TPI-1 相关产品
| 产品描述 | TPI-1 is a SHP-1 inhibitor. |
| 靶点活性 | SHP1:40 nM. |
| 体外活性 | SHP-1被认为是潜在的癌症治疗靶标。TPI-1在10 ng/mL的浓度开始有效地增加SHP-1磷酸化底物pLck-pY394。TPI-1在Jurkat T细胞中选择性地增加SHP-1磷酸化底物(pLck-pY394、pZap70和pSlp76),对pERK1/2或pLck-pY505的影响较小。TPI-1诱导小鼠脾脏产生IFNγ+细胞,并在人类外周血中诱导IFNγ+细胞[1]。 |
| 体内活性 | TPI-1通过口服可耐受剂量在T细胞依赖的方式下抑制小鼠中B16黑素瘤肿瘤的生长,但对体外培养的B16细胞生长影响不大。同时,TPI-1在小鼠体内增加了pLck-pY394和IFNγ+细胞的数量。TPI-1还作为一个可耐受的皮下(s.c.)药剂,抑制了B16肿瘤的生长并延长了肿瘤小鼠的生存时间[1]。 |
| 激酶实验 | Jump-In TI CHO-K cells stably expressing WT or mutant S1P3 are serum-starved for 4 hrs. They are then incubated at 4 °C for 30 min in the binding buffer containing 20 mM Tris-HCl (pH 7.5), 100 mM NaCl, 15 mM NaF, 0.5 mM EDTA, 1 mM Na3VO4, 0.5% fatty acid-free bovine serum albumin, and protease inhibitor mixture with 0.1 nM [33P]S1P and increasing concentrations of S1P, SPM-242, or CYM-5541. Cells are washed three times with cold binding buffer. Cell-bound radioactivity is measured by lysing the cells with 0.5% SDS followed by liquid scintillation counting. The raw data is normalized so that the level of [33P]S1P bound to each cell line (WT or mutant) in the absence of competing ligand is referenced as 100% for its own cell line[1]. |
| 别名 | TPI1, TPI 1 |
| 分子量 | 253.08 |
| 分子式 | C12H6Cl2O2 |
| CAS No. | 79756-69-7 |
| Smiles | Clc1ccc(Cl)c(c1)C1=CC(=O)C=CC1=O |
| 密度 | no data available |
| 颜色 | Yellow |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 45 mg/mL (177.81 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.9 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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