1. Protein Tyrosine Kinase/RTK
  2. Insulin Receptor
  3. Kaempferitrin

Kaempferitrin (Synonyms: Lespedin; Lespenephryl)

Cat. No.: HY-N0628 Purity: 99.12%
Handling Instructions

Kaempferitrin is a natural flavonoid, possesses antinociceptive, anti-inflammatory, anti-diabetic, antitumoral and chemopreventive effects, and activates insulin signaling pathway.

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

Kaempferitrin Chemical Structure

Kaempferitrin Chemical Structure

CAS No. : 482-38-2

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10 mM * 1 mL in DMSO USD 178 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 140 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Kaempferitrin is a natural flavonoid, possesses antinociceptive, anti-inflammatory, anti-diabetic, antitumoral and chemopreventive effects, and activates insulin signaling pathway.

IC50 & Target

Insulin Receptor[1]

In Vitro

Kaempferitrin activates insulin signaling pathway. Kaempferitrin causes survival rates higher than 90% at 1-20 μM in matured 3T3-L1 adipocyte, and the survival rates decline rapidly at 25 and 50 μM. Kaempferitrin (15 μM) increases insulin receptor beta tyrosine phosphorylation and tyrosine phosphorylation of the insulin receptor substrate 1, and such effects are similar to that of 10 nM insulin. Kaempferitrin (15 μM) also stimulates akt phosphorylation on ser473, and the stimulation can be blocked by a PI3-K inhibitor wortmannin. Kaempferitrin potently exerts the translocation of GLUT4 to the membrane of adipocytes at 15 μM, and this is suppressed by wortmannin. In addition, Kaempferitrin increases the total levels of Glu4 protein in differentiated cells and secreted adiponectin in mature 3T3-L1 adipocytes[1]. Kaempferitrin is cytotoxic to human cancer cells such as HeLa and MDA-MB231 cells, with IC50s of 45 ± 2.6 and 65 ± 2.6 μM, and shows low toxic effects on non-tumorigenic cells. Kaempferitrin (45 μM) induces apoptosis of HeLa cells after treatment for 24 and 48 h, and causes reactive oxygen species (ROS) generation in HeLa cells. Furthermore, Kaempferitrin (45 μM) exerts G1 arrest, causes the expression of proteins associated with intrinsic pathway of apoptosis and activates caspase 3 in HeLa cells[2].

In Vivo

Kaempferitrin (2.5, 10 and 25 mg/kg, i.p.) markedly suppresses the growth of tumor by 40%, 87% and 97%, and decreases tumor weight by 37%, 81% and 95%, respectively in nu/nu mice bearing HeLa tumor. Kaempferitrin also inhibits cell proliferation and extends life span in mice bearing tumor[2].

Molecular Weight

578.52

Formula

C₂₇H₃₀O₁₄

CAS No.

482-38-2

SMILES
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (216.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7285 mL 8.6427 mL 17.2855 mL
5 mM 0.3457 mL 1.7285 mL 3.4571 mL
10 mM 0.1729 mL 0.8643 mL 1.7285 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.60 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.60 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.60 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Viability assay is carried out by MTT assay. Preconfluent 3T3-L1 preadipocytes are seeded to reach confluence. Kaempferitrin is added in replacement of insulin immediately after confluence (day 0), and the viability is measured 3 h after addition of the compound. Another cell viability assay is performed at day 8. For kaempferitrin combined with insulin treatment, various concentrations of kaempferitrin are added simultaneously with 0.2 nM insulin from day 0 to day 8. Cells without insulin or kaempferitrin treatment during differentiation (day 0 to day 8) are used as control. Finally, to verify the cell viability in matured 3T3-L1 cells treated with insulin or kaempferitrin for 24-48 h, MTT are incubated for 3 h at the end of the 24 h and 48 h period of compound treatments, and survival rates calculated and compared to that without insulin or kaempferitrin[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

The nu/nu mice are injected subcutaneously in their backs with HeLa cells (1.5 × 106). Four hours after tumor implantation, groups of five mice receive doses of Kaempferitrin between 2.5 to 25 mg/kg, dissolved in 0.1 mL of 0.9% saline solution, cisplatin (CDDP) 1 mg/kg or paclitaxel (PCX) 1 mg/kg injected intraperitoneally daily over a period of 32 days. The animal control group received 0.1 mL of vehicle solution. Tumors are measured using a vernier caliper, and their size in mm3 is calculated Tumor volume = lenght × width × height2. At the end of the experiments, animals are sacrificed and their tumors are excised and weighed[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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