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Wogonin CDK inhibitor

Cat.No.S4743

Wogonin (Vogonin), a natural and biologically-active flavonoid found in plants, is an inhibitor of CDK9 and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity; This compound also inhibits N-acetyltransferase.
Wogonin CDK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 284.26

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RAW264.7 cells  Function assay Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW264.7 cells by enzyme immunoassay, IC50=1.07 μM
SW1353 cells Function assay Antiinflammatory activity in PMA-stimulated human SW1353 cells assessed as inhibition of NF-kappaB activation, IC50=39 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 284.26 Formula

C16H12O5

Storage (From the date of receipt)
CAS No. 632-85-9 Download SDF Storage of Stock Solutions

Synonyms Vogonin Smiles COC1=C(C=C(C2=C1OC(=CC2=O)C3=CC=CC=C3)O)O

Solubility

In vitro
Batch:

DMSO : 56 mg/mL ( (197.0 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
CDK9 [1]
N-acetyltransferase [5]
In vitro
Wogonin inhibits PMA-induced COX-2 gene expression by inhibiting c-Jun expression and AP-1 activation in A549 cells[1]. This compound is an inhibitor of cyclin-dependent kinase 9 (CDK9) and block phosphorylation of the carboxy-terminal domain of RNA polymerase II at Ser. Thus, it reduces RNA synthesis and subsequently rapid downregulation of the short-lived anti-apoptotic protein myeloid cell leukemia 1 (Mcl-1) resulting in apoptosis induction in cancer cells. It directly binds to CDK9, presumably to the ATP-binding pocketa and does not inhibit CDK2, CDK4 and CDK6 at doses that inhibit CDK9 activity. This chemical preferentially inhibits CDK9 in malignant compared with normal lymphocytes. It is a also potent anti-oxidant capable to scavenge •O2− [2]. This compound significantly inhibits the translocation of NFATc1 from the cytoplasm to the nucleus and its transcriptional activation activity. It also significantly inhibits osteoclast differentiation and decreases the transcription of osteoclast‑associated immunoglobulin‑like receptor, tartrate‑resistant acid phosphatase and calcitonin receptor[4]. It Inhibits N-acetyltransferase Activity[5].
In vivo
Wogonin suppresses growth of human cancer xenografts in vivo. At doses lethal to tumor cells, this compound shows no or little toxicity for normal cells and had also no obvious toxicity in animals[2]. It could induce apoptosis in murine sarcoma S180 thereby inhibiting the tumor growth both in vitro and in vivo[3]. An intraperitoneal injection of 200 mg/kg of this chemical could completely inhibit leukemia and CEM cells[4].
References
  • https://pubmed.ncbi.nlm.nih.gov/26622440/
  • https://pubmed.ncbi.nlm.nih.gov/15816529/

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