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Technical Data
| Formula | C16H19N5 |
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| Molecular Weight | 281.36 | CAS No. | 172889-26-8 | |
| Solubility (25°C)* | In vitro | DMSO | 5 mg/mL (17.77 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | PP1 (AGL 1872, EI 275) is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM. | ||||||||
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| In vitro | PP1 is a nano-molar inhibitor of Lck and FynT, inhibits anti-CD3-induced protein-tyrosine kinase activity in T cells (IC50, 0.5 μM), demonstrates selectivity for Lck and FynT over ZAP-70, and preferentially inhibits T cell receptor-dependent anti-CD3-induced T cell proliferation (IC50, 0. 5 μM) over non-T cell receptor-dependent phorbol 12-myristate 13-acetate/interleu-kin-2 (IL-2)-induced T cell proliferation. PP1 (1 μM) selectively inhibits the induction of the IL-2 gene, but not the granulocyte-macrophage colony-stimulating factor or IL-2 receptor genes. PP1 also inhibits Src (IC50, 170 nM) and Hck (IC50, 20 nM). PP1 is 50–100-fold less active in the inhibition of A-431 epidermal growth factor receptor autophosphorylation (IC50, 0.25 μM). [1] PP1 also inhibits Kit and Bcr-Abl tyrosine kinases with IC50 of ∼75 nM and 1 μM, respectively. PP1 completely abrogates the proliferation of M07e cells in response to SCF with IC50 of 0.5–1 μM. PP1 (1 μM) inhibits SCF-induced c-Kit autophosphorylation in intact cells and blocks the activation of mitogen-activated protein kinase and Akt. PP1 inhibits the activity of mutant constitutively active forms of c-Kit (D814V and D814Y) found in mast cell disorders, and triggers apoptosis in the rat basophilic leukemia cell line RBL-2H3 that expresses mutant c-Kit. PP1 reduces the constitutive activation of signal transducer and activators of transcription 5 and mitogen-activated protein kinase and triggeres apoptosis in FDCP1 cells expressing Bcr-Abl. [2] |
Protocol (from reference)
References
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Customer Product Validation
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Data from [Data independently produced by J Virol, 2011, 85(5), 2296-303]
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Data from [Data independently produced by , , Theranostics, 2018, 8(2):384-398]
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Data from [Data independently produced by , , Kidney Int, 2018, 93(1):173-187]
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Data from [Data independently produced by , , Oncol Rep, 2016, 36(2):1000-6]
Selleck's PP1 has been cited by 26 publications
| Engineering tumoral vascular leakiness with gold nanoparticles [ Nat Commun, 2023, 14(1):4269] | PubMed: 37460554 |
| Engineering tumoral vascular leakiness with gold nanoparticles [ Nat Commun, 2023, 186(22):4851-4867.e20] | PubMed: 37460554 |
| Young and undamaged recombinant albumin alleviates T2DM by improving hepatic glycolysis through EGFR and protecting islet β cells in mice [ J Transl Med, 2023, 21(1):89] | PubMed: 36747238 |
| Casein kinase 1 controls the shuttling of epidermal growth factor receptor and estrogen receptor in endometrial carcinoma induced by breast cancer hormonal therapy: Relevance of GPER1/Src [ Cell Signal, 2023, 108:110733] | PubMed: 37257767 |
| Brain-Derived Neurotrophic Factor regulates LYN kinase mediated Myosin Light Chain Kinase activation to modulate non-muscle myosin II activity in hippocampal neurons [ J Biol Chem, 2022, S0021-9258(22)00494-X] | PubMed: 35598826 |
| Peroxisomal-derived ether phospholipids link nucleotides to respirasome assembly [ Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z] | PubMed: 33723432 |
| Siglec-8 Signals Through a Non-Canonical Pathway to Cause Human Eosinophil Death In Vitro [ Front Immunol, 2021, 12:737988] | PubMed: 34721399 |
| Secreted Pyruvate Kinase M2 Promotes Lung Cancer Metastasis through Activating the Integrin Beta1/FAK Signaling Pathway. [ Cell Rep, 2020, 30(6):1780-1797] | PubMed: 32049010 |
| CXCR7 promotes melanoma tumorigenesis via Src kinase signaling. [ Cell Death Dis, 2019, 10(3):191] | PubMed: 30804329 |
| SRC and ERK cooperatively phosphorylate DLC1 and attenuate its Rho-GAP and tumor suppressor functions. [ J Cell Biol, 2019, 218(9):3060-3076] | PubMed: 31308216 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.