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Technical Data
| Formula | C24H27N7O |
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| Molecular Weight | 429.52 | CAS No. | 1594092-37-1 | |
| Solubility (25°C)* | In vitro | DMSO | 85 mg/mL (197.89 mM) | |
| Ethanol | 33 mg/mL (76.82 mM) | |||
| Water | 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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Preparing Stock Solutions
Biological Activity
| Description | AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM in a cell-free assay, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively. | ||||
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| Targets |
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| In vitro | AZ191 selectively inhibits DYRK1B serine/threonine kinase activity with no effect on tyrosine kinase autophosphorylation. In HEK-293 cells, AZ191 also displays much greater potency for DYRK1B over DYRK1A, inhibiting CCND1 phosphorylation. In HD1B cells, AZ191 strongly inhibits the levels of the cell-cycle regulators, p21Cip1 and p27Kip1, and increases cell-cycle progression. [1] |
Protocol (from reference)
Customer Product Validation
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, , Cell Death Dis, 2014, 5:e1548.
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Data from [Data independently produced by , , Sci Rep, 2016, 6:37052.]
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Data from [Data independently produced by , , Oncotarget, 2017, 8(1):833-845]
Selleck's AZ191 has been cited by 11 publications
| A DYRK1B-dependent pathway suppresses rDNA transcription in response to DNA damage [ Nucleic Acids Res, 2021, gkaa1290] | PubMed: 33469661 |
| TROAP switches DYRK1 activity to drive hepatocellular carcinoma progression [ Cell Death Dis, 2021, 12(1):125] | PubMed: 33500384 |
| TROAP switches DYRK1 activity to drive hepatocellular carcinoma progression [ Cell Death Dis, 2021, 12(1):125] | PubMed: 33500384 |
| Pharmacologic and genetic approaches define human pancreatic β cell mitogenic targets of DYRK1A inhibitors. [ JCI Insight, 2020, 5(1)] | PubMed: 31821176 |
| Serum deprivation initiates adaptation and survival to oxidative stress in prostate cancer cells [ Sci Rep, 2020, 10(1):12505] | PubMed: 32719369 |
| Targeting DYRK1B suppresses the proliferation and migration of liposarcoma cells [ Oncotarget, 2018, 9(17):13154-13166] | PubMed: 29568347 |
| Inhibitors of dual-specificity tyrosine phosphorylation-regulated kinases (DYRK) exert a strong anti-herpesviral activity. [Hutterer C, et al. Antiviral Res, 2017, 143:113-121] | PubMed: 28400201 |
| DYRK1B blocks canonical and promotes non-canonical Hedgehog signaling through activation of the mTOR/AKT pathway. [Singh R, et al. Oncotarget, 2017, 8(1):833-845] | PubMed: 27903983 |
| Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells [Li Z, et al. Cancer Lett, 2016, 370(2):332-44] | PubMed: 26586345 |
| Bafilomycin A1 induces caspase-independent cell death in hepatocellular carcinoma cells via targeting of autophagy and MAPK pathways. [Yan Y, et al. Sci Rep, 2016, 6:37052] | PubMed: 27845389 |
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.