TPI-1 is a SHP-1 inhibitor, inhibits recombinant SHP-1 with an IC50 of 40 nM. TPI-1 is effective starting at 10 ng/mL in increasing SHP-1 phospho-substrates pLck-pY394. TPI-1 selectively increases SHP-1 phospho-substrates (pLck-pY394, pZap70 and pSlp76) in Jurkat T cells but has little effects on pERK1/2 or pLck-pY505.
In vivo, TPI-1 inhibits the growth of B16 melanoma tumors in mice at a tolerated oral dose in a T cell-dependent manner but has little effects on B16 cell growth in culture. TPI-1 thus also increases pLck-pY394 and IFNγ+ cells in mice.
| Molecular Weight | 253.08 |
| Formula | C12H6Cl2O2 |
| CAS Number | 79756-69-7 |
| Solubility (25°C) | DMSO ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Phosphatase Products |
|---|
| M5N36
M5N36 is a potent and selective Cdc25C inhibitor with IC50 values of 0.15, 0.19, 0.06 µM for Cdc25A, Cdc25B, Cdc25C, respectively. |
| DPM-1003
DPM-1003 is an orally potent, specific inhibitor of PTP1B. |
| D-3
D-3, a phosphorpeptide, is an efficient, simple, and specific iPSC-eliminating agent. |
| EGF Receptor Substrate 2 (Phospho-Tyr5)
EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. |
| Calcineurin autoinhibitory peptide
Calcineurin autoinhibitory peptide is a selective inhibitor of Ca2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
