1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
    MAPK/ERK Pathway
  2. CDK
    ERK
  3. Bohemine

Bohemine 

Cat. No.: HY-12843
Handling Instructions

Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities.

For research use only. We do not sell to patients.

Bohemine Chemical Structure

Bohemine Chemical Structure

CAS No. : 189232-42-6

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Description

Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities[1][2].

IC50 & Target[2]

CDK2/cyclinE

4.6 μM (IC50)

cdk2/cyclin A

83 μM (IC50)

CDK9/cyclinT1

2.7 μM (IC50)

ERK2

52 μM (IC50)

In Vitro

Bohemine (0-30 µM; 72 hours; ME-750 cells) treatment inhibits cell growth. Addition of Bohemine at concentrations in the range of 1-10 µM results in a short-term arrest of growth and of monoclonal antibody production. The short-term suppression of cell functions is followed by a significant temporary increase of specific growth rate and of specific production rate[1].
Hybridoma cells are retarded both at the G1/S boundary and at the G2/M boundary, depending on Bohemine (0-30 µM) concentration[1].
T-lymphoblastic cell line CEM is treated by Bohemine, five proteins are found to be downregulated, namely α-enolase, triosephosphate isomerase, initiation factor 5A, and α- and β-subunits of Rho GDP-dissociation inhibitor 1. These proteins play significant roles in glycolysis, proteosynthesis, and in cytoskeleton rearrangement[1].
Bohemine inhibits growth of human tumor cell lines with an IC50 of 27 µM[2].

Cell Viability Assay[1]

Cell Line: Mouse hybridoma ME-750 cells
Concentration: 0 µM, 1 µM, 3 µM, 10 µM and 30 µM
Incubation Time: 72 hours
Result: At 10 µM and 30 µM concentrations, the viable cell count was significantly lower with respect to control, i.e., 77% and 48%, respectively.
In Vivo

Bohemine (50 mg/kg; intravenous injection; BALB/c mice) treatment shows Cmax is 72,308 nM, observed clearance is 0.23 L/h and T1/2 is 1.39 h[2].

Animal Model: BALB/c mice bearing the colon 26 murine tumor[2]
Dosage: 50 mg/kg
Administration: Intravenous injection (Pharmacokinetic Analysis)
Result: Cmax is 72,308 nM, observed clearance is 0.23 L/h and T1/2 is 1.39 h.
Molecular Weight

340.42

Formula

C₁₈H₂₄N₆O

CAS No.

189232-42-6

SMILES

OCCCNC1=NC(NCC2=CC=CC=C2)=C3N=CN(C(C)C)C3=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BohemineCDKERKCyclin dependent kinaseExtracellular signal regulated kinasesCdk2/cyclin ECdk2/cyclin Adk9/cyclin T1purineMAbanti-cancerproteosynthesiscytoskeletonrearrangementInhibitorinhibitorinhibit

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