DHI1
DHI1 is an anti-leukemia agent with high selectivity for Jurkat (IC50 = 21.83 μM) and HL-60 (IC50 = 19.14 μM) leukemia cells and has low toxicity to non-cancerous cells. DHI1 can induce G2/M phase cell arrest in Jurkat and HL-60 leukemia cells, as well as S phase arrest in HL-60 cells, and has significant effects on cell cycle signaling molecules Wee1, cyclin B1, cdc2 on Tyr15, and Chk1. DHI1 inhibits the migration and invasion of Jurkat and HL-60 cells by disrupting cytoskeletal actin filaments. DHI1 can be used to study hematological malignancies.
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- Formule: C18H15BrN2O
- Masse moléculaire:355.23
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chk1 |
DHI1 (Compound 4a) (3-100 μM, 24-72 h) shows inhibitory viability against Jurkat and HL-60 cells, with IC50s of 21.83 and 19.14 μM, but has weak inhibitory viability against HCT-116, HeLa, MCF-7, U87,Hep G2, A549, A2780, BJ-5ta, MCF-10A cells[1].
DHI1 (19.14-21.83 μM, 24-72 h) induces cell cycle arrest at G2/M phase and affects signaling proteins related to the cell cycle in Jurkat and HL-60 cells[1].
DHI1 (10-40 μM, 3 h) decreases chemotaxis and invasiveness of Jurkat and HL-60 leukemic cells[1].
DHI1 (19.14-21.83 μM, 24-72 h) induces disruption, disorganization, damage to F-actin structures and nuclear fragmentation and membrane blebbing, impacts cytoskeleton of Jurkat and HL-60 leukemic cells[1].
DHI1 (3.125-100 μM, 24 h) enhances PBMC cell viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat cells
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Concentration:21.83 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Induced cell cycle arrest at G2/M phase at 24 h and increases sub-G0/G1 fraction. Reduced phosphorylation of Wee1 (Ser642) , cyclin B1 (Ser133), cdc2 on Tyr15, human retinoblastoma protein (Rb) .
Increased phosphorylation of Chk1 (Ser345), but reduced phosphorylation of Chk1 (Ser345) after 72 hours.
Increased the level of p21 at 24 and 48 h.
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Cell Line:HL-60 cells
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Concentration:19.14 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Induced cell cycle arrest at G2/M phase after 24 h, blocked S phase, and increased sub-G0/G1 peak of DNA fragmentation.
Reduced phosphorylation of Wee1 (Ser642), cdc2 on Tyr15, human retinoblastoma protein (Rb), increased phosphorylation of Chk1 (Ser345).
Increased the level of p21 at 24 h, but decrease p21 at 48-72 h.
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Cell Line:Jurkat and HL-60 cells
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Concentration:10, 20, and 40 μM
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Incubation Time:3 h
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Result:Decreased relative cell chemotaxis by 31.1 and 45.7% at 40 μM, reduced HL-60 cell invasion by 17.7% at 20 μM.
Induced concentration-dependent effects on the invasiveness/motility, reduced cell invasion by 39.7 and 57.8% at 40 μM, reduced HL-60 cell invasion by 33.6% at 20 μM.
Chemical Information
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Masse moléculaire 355.23
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Formule C18H15BrN2O
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SMILES
CN1C=C(C2=CC=CC=C21)C3CC(C4=CC=C(Br)C=C4)=NO3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DHI1 Related Classifications
HY-175261 Related Classifications
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