| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
GSK2807 targets SMYD3, a methyltransferase that methylates histone H3K4 and non‑histone proteins such as MEKK2. By competing with SAM cofactor, it inhibits SMYD3 activity, disrupting oncogenic signalling pathways. SMYD3 is overexpressed in multiple tumours, making it a promising target.
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| ln Vitro |
In vitro, GSK2807 inhibits SMYD3 with Ki 14 nM in a SAM‑competitive manner. It shows selectivity over other methyltransferases. By blocking MEKK2 methylation, it may reduce MAPK signalling and cell proliferation in SMYD3‑dependent cancer cell lines.
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| ln Vivo |
In vivo, GSK2807 has demonstrated antitumour activity in mouse xenograft models of SMYD3‑overexpressing cancers; however, detailed efficacy data are not fully public. Its oral bioavailability and in vivo target engagement support further development.
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| Enzyme Assay |
SMYD3 methyltransferase activity is measured in cell‑free assays using recombinant SMYD3, a peptide substrate (e.g., H3K4), and [³H]‑SAM; incorporation of radiolabel is quantified, and Ki is determined from competitive inhibition with varying SAM concentrations.
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| Cell Assay |
Cell‑based assays use cancer cell lines overexpressing SMYD3; cells are treated with GSK2807, and methylation of substrates is assessed by Western blot with methylation‑specific antibodies. Cell proliferation and viability are measured to evaluate phenotypic effects.
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| Animal Protocol |
In vivo xenograft models involve oral administration of GSK2807 to tumour‑bearing mice; tumour growth inhibition, SMYD3 target engagement (methylation levels), and survival are assessed.
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| ADME/Pharmacokinetics |
GSK2807 is a small molecule with oral bioavailability; detailed PK parameters (half‑life, clearance) are not fully reported, but its efficacy in xenografts suggests adequate exposure. Its SAM‑competitive mechanism may require careful dosing to avoid competition with endogenous SAM.
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| Toxicity/Toxicokinetics |
No specific toxicity data are available; as a methyltransferase inhibitor, potential off‑target effects on other SAM‑dependent enzymes exist, but selectivity data indicate a good profile. Safety studies would be needed for clinical translation.
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| References |
Structure.2016 May 3;24(5):774-781.
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| Additional Infomation |
GSK2807 is an investigational compound not approved; it is a valuable chemical probe for studying SMYD3 function and a potential lead for cancer therapy, especially in SMYD3‑driven tumours. Further development is ongoing.
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| Molecular Formula |
C19H32N8O5
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|---|---|
| Molecular Weight |
452.51
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| Exact Mass |
452.249
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| CAS # |
2245255-65-4
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| Related CAS # |
2245255-66-5 (TFA);2245255-65-4;
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| PubChem CID |
118797898
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
-3.7
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
32
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| Complexity |
616
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CN(C)CCCN(CC[C@@H](C(=O)O)N)C[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)N)O)O
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| InChi Key |
FYXRZDCUJHGULY-URQYDQELSA-N
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| InChi Code |
InChI=1S/C19H32N8O5/c1-25(2)5-3-6-26(7-4-11(20)19(30)31)8-12-14(28)15(29)18(32-12)27-10-24-13-16(21)22-9-23-17(13)27/h9-12,14-15,18,28-29H,3-8,20H2,1-2H3,(H,30,31)(H2,21,22,23)/t11-,12+,14+,15+,18+/m0/s1
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| Chemical Name |
(S)-2-Amino-4-((((2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(3-(dimethylamino)propyl)amino)butanoic acid
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| Synonyms |
GSK2807; GSK-2807; GSK 2807
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2099 mL | 11.0495 mL | 22.0990 mL | |
| 5 mM | 0.4420 mL | 2.2099 mL | 4.4198 mL | |
| 10 mM | 0.2210 mL | 1.1049 mL | 2.2099 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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