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Chemical Structure : LDN-192960 hydrochloride
CAS No.: 2309172-48-1
Catalog No.: PC-73113Not For Human Use, Lab Use Only.
LDN192960 (LDN 192960) is a highly potent and selective DYRK2 inhibitor with IC50 of 13 nM toward DYRK2 at 50 uM ATP.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $248 | In stock | |
| 25 mg | $428 | In stock | |
| 100 mg | $1080 | In stock | |
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| 1 g | Get quote |
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LDN192960 (LDN 192960) is a highly potent and selective DYRK2 inhibitor with IC50 of 13 nM toward DYRK2 at 50 uM ATP.
LDN192960 suppresses Thr25 RPT3 phosphorylation in a dose-dependent manner in HEK293T cells transiently overexpressing DYRK2-FLAG, with maximal effects at 1-10 uM.
LDN192960 does not inhibit any of the 130+ kinases including other CMGC kinase family members that are closely related to the DYRKs.
LDN192960 binds to the ATP-binding pocket of DYRK2, also potently inhibits DYRK1A, DYRK3 and Pim with IC50 of <3, 122 and 10 nM, respectively.
LDN192960 perturbs proteasome activity, induces cell death, and impedes proliferation and invasion on MDA-MB-468 cells.
LDN192960 impedes MM progression and delays myeloma-mediated bone degeneration.
LDN192960 induces cytotoxicity in bortezomib-resistant MM, both in cells and in vivo. significantly alleviates tumor burden in standard and PDX TNBC models.
| M.Wt | 401.35 | |
| Formula | C18H22Cl2N2O2S | |
| Appearance | Solid | |
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1. Banerjee S, et al. Proc Natl Acad Sci U S A. 2019 Dec 3;116(49):24881-24891.
2. Correa-Sáez A, et al. Cell Mol Life Sci. 2020 Dec;77(23):4747-4763.
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