| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Source | Plant — Guttiferae Garcinia kola Heckel |
| Molecular weight | |
| Molecular formula | C31H24O12 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Kolaflavanone is a biflavonoid allosteric inhibitor of Eg5. It inhibits the ATPase and tyrosinase activities of Eg5 under both basal and microtubule-activated conditions, suppresses microtubule sliding activity, binds the L5/α2/α3 allosteric pocket of Eg5, and induces conformational changes in Eg5 together with microtubule dissociation. It also interacts with aldehyde dehydrogenase, inhibits the ATPase activity of kinesin-1, and binds HSA through pH-dependent forces. In addition, Kolaflavanone exhibits antihepatotoxic activity and can be used in studies of Phalloidin-induced liver injury[1][2][3]. It is a biflavone flavonoid derived from the plant Garcinia kola (Guttiferae), with a molecular formula of C31H24O12 and a molecular weight of 588.52 g/mol.
Physical & Chemical Properties
| CAS Number | 68705-66-8 |
|---|---|
| Molecular Formula | C31H24O12 |
| Molecular Weight | 588.52 g/mol |
| Structure Classification | Flavonoids Biflavones |
| SMILES | O=C1[C@@H]([C@H](OC2=CC(O)=CC(O)=C12)C3=CC=C(C=C3)O)C4=C5C(C([C@@H]([C@H](O5)C6=CC=C(C(O)=C6)OC)O)=O)=C(C=C4O)O |
| Target | Eg5 |
| Signaling Pathway | Cell Cycle/DNA Damage; Cytoskeleton |
| Initial Source | Plant — Guttiferae Garcinia kola Heckel |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. Iwu MM. Antihepatoxic constituents of Garcinia kola seeds. Experientia. 1985 May 15;41(5):699-700.
[3]. Kolawole AO, et al. Kolaflavanone of kolaviron selectively binds to subdomain 1B of human serum albumin: spectroscopic and molecular docking evidences. Computational Toxicology. 2020;13:100118.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
The basal ATPase activity of the recombinant mouse Eg5 motor domain is inhibited by Kolaflavanone (KLF) (0-250 μM; 20 min), with an IC50 of 98 μM[1]. Microtubule-activated ATPase activity of the recombinant mouse Eg5 motor domain is inhibited by Kolaflavanone (0-250 μM), with an IC50 of 125 μM[1]. Kolaflavanone (100-150 μM; 900 s) lowers the microtubule sliding rate of the recombinant mouse Eg5 motor domain by approximately 53% at 100 μM and approximately 59% at 150 μM, and induces microtubules to dissociate from Eg5[1]. As an allosteric inhibitor of the recombinant mouse Eg5 motor domain, Kolaflavanone (100 μM) suppresses ATPase activity while not competing directly for ATP or for microtubule-binding sites[1]. In preference to the conventional kinesin-1 motor domain, Kolaflavanone (100-150 μM) inhibits the ATPase activity of the recombinant mouse Eg5 motor domain that is activated by microtubules, and lowers Eg5 activity by 62% at 150 μM[1]. The L5/α2/α3 allosteric pocket of the recombinant mouse Eg5 motor domain is bound stably by Kolaflavanone, which forms hydrogen bonds to the residues Glu118, Tyr211 and Arg221 and induces conformational changes that lessen the flexibility of Eg5 and decrease the solvation degree of the allosteric pocket[1]. Via a static quenching mechanism, Kolaflavanone (0-62.50 μM; 15-40 °C) binds to human serum albumin (HSA), with a single binding site and moderate affinity (binding constant: 3.13-8.44 × 103 L·mol-1). Affinity falls as temperature rises, which lowers the binding rate of HSA at high temperatures[3]. In human serum albumin (HSA), the fluorescence of tyrosine and tryptophan residues is quenched by Kolaflavanone (0-56.25 μM; 25 °C), and the hydrophobic microenvironment of these residues is not altered at 25 °C[3]. Non-radiative fluorescence resonance energy transfer occurs between Kolaflavanone and human serum albumin (HSA) at 25 °C, with a binding distance of 3.64 nm under conditions of 25 °C and pH 7.4[3].
In Vivo
In female Swiss mice, Kolaflavanone (KLF) (10-50 mg/kg; i.p.; single administration) shows dose-dependent hepatoprotective activity against lethal liver injury induced by phalloidin, reaching a 100% survival rate at 50 mg/kg by intraperitoneal injection[2].
| Animal Model | Swiss mice (female, average weight 24 g, challenged with intraperitoneal phalloidin)[2] |
|---|---|
| Dosage | 10 mg/kg; 50 mg/kg |
| Administration | i.p.; single dose |
| Result | Resulted in a 35% survival rate in phalloidin-challenged mice at 10 mg/kg. Resulted in a 100% survival rate in phalloidin-challenged mice at 50 mg/kg. Showed statistically significant differences compared to toxin and vehicle control groups (p = 0.05). |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
- Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).
Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).
