2. Cell Cycle/DNA Damage
  3. CDK Wee1 Checkpoint Kinase (Chk)
  4. 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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DHI1

DHI1 Chemical Structure

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DHI1 Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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PKMYT1

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Chk1 Chk2 BUBR1

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Description

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[1].

IC50 & Target[1]

Chk1

 

In Vitro

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.

DHI1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: Jurkat cells
Concentration: 21.83 μM
Incubation Time: 24 h, 48 h, 72 h
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.

Cell Cycle Analysis[1]

Cell Line: HL-60 cells
Concentration: 19.14 μM
Incubation Time: 24 h, 48 h, 72 h
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.

Cell Migration Assay [1]

Cell Line: Jurkat and HL-60 cells
Concentration: 10, 20, and 40 μM
Incubation Time: 3 h
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.
Molecular Weight

355.23

Formula

C18H15BrN2O
SMILES

CN1C=C(C2=CC=CC=C21)C3CC(C4=CC=C(Br)C=C4)=NO3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DHI1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DHI1DHI 1DHI-1CDKWee1Checkpoint Kinase (Chk)Cyclin dependent kinaseHematological malignanciesJurkat cellsHL-60 cellsInhibitorinhibitorinhibit

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