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ULK1-IN-2
CAS No. 2497409-01-3
ULK1-IN-2( —— )
Catalog No. M35716 CAS No. 2497409-01-3
ULK1-IN-2 is a potent ULK1 inhibitor with potential anticancer activity, inducing apoptosis while blocking autophagy.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 78 | Get Quote |
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| 5MG | 116 | Get Quote |
|
| 10MG | 188 | Get Quote |
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| 25MG | 419 | Get Quote |
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| 50MG | 635 | Get Quote |
|
| 100MG | 1008 | Get Quote |
|
| 500MG | 2007 | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
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Product NameULK1-IN-2
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NoteResearch use only, not for human use.
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Brief DescriptionULK1-IN-2 is a potent ULK1 inhibitor with potential anticancer activity, inducing apoptosis while blocking autophagy.
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DescriptionULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer).
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In VitroULK1-IN-2 (compound 3s) (10 μM, 24 h) shows strong anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7.ULK1-IN-2 (0-8 μM, 24 h) blocks autophagy via inhibiting ULK1 in A549 cells.ULK1-IN-2 (0-8 μM, 24 h) induces apoptosis via the mitochondrial pathways in A549 cells in dose department manner.ULK1-IN-2 (0-8 μM, 24 h) inhibits ULK1 and p-ULK1ser317 expression in a concentration-dependent manner, remarkably decreases Bcl-2 expression, increases Bax and the active form of Caspase-3 expression.Cell Proliferation Assay Cell Line:Human cancer cell lines A549, U937, HL60, MDA-MB-468 and MCF-7 Concentration: 10 μM Incubation Time:24 h Result:Significantly improved anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7, with kinase inhibitory activity of 99.15% and IC50 values of 1.94, 12.92, 10.89, 16.83, and 19.60 μM, respectively.Cell Autophagy Assay Cell Line:A549 cells Concentration:0, 2, 4, 8 μM Incubation Time:24 h Result:Blocked autophagy of A549 cells via inhibiting ULK.Western Blot Analysis Cell Line:A549 cells Concentration:0, 2, 4, 8 μM Incubation Time:24 h Result:Inhibited expression of ULK1 and p-ULK1ser317 in a concentration-dependent manner. Increased the autophagy substrate P62, reduced LC3-I conversion to LC3-II, and decreased the levels of Beclin1. Remarkably decreased Bcl-2 expression, increased Bax and the active form of Caspase-3 expression.
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In Vivo——
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Synonyms——
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PathwayAutophagy
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TargetAutophagy
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RecptorAutophagy | Apoptosis
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Research Area——
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Indication——
Chemical Information
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CAS Number2497409-01-3
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Formula Weight495.26
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Molecular FormulaC19H16BrFN4O6
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 33.33 mg/mL (67.30 mM; Ultrasonic )
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SMILESO(C)C1=C(OC)C=C(NC=2N=C(OC3=C(F)C=C(N(=O)=O)C=C3)C(Br)=CN2)C=C1OC
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Sun D, Yang Z, Zhen Y, et al. Discovery of 5-bromo-4-phenoxy-N-phenylpyrimidin-2-amine derivatives as novel ULK1 inhibitors that block autophagy and induce apoptosis in non-small cell lung cancer. Eur J Med Chem. 2020;208:112782.?
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