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BAY 598 is a potent and selective competitive inhibitor of SMYD2 lysine methyltransferase, IC50 values are 27 and 58 nM for biochemical and cellular activity assays, respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $43 | In Stock | |
5 mg | $88 | In Stock | |
10 mg | $142 | In Stock | |
25 mg | $263 | In Stock | |
50 mg | $428 | In Stock | |
100 mg | $645 | In Stock | |
1 mL x 10 mM (in DMSO) | $98 | In Stock |
Description | BAY 598 is a potent and selective competitive inhibitor of SMYD2 lysine methyltransferase, IC50 values are 27 and 58 nM for biochemical and cellular activity assays, respectively. |
Targets&IC50 | SMYD2:27 nM |
In vitro | METHODS: PDAC cells SW1990 and MIA PaCa2 were treated with BAY-598 (10 µM) and doxorubicin (1 µM) for 48 h. Cell viability was determined by MTT assay. RESULTS: PDAC cells were highly sensitive to acute treatment with the low-dose combination of doxorubicin and BAY-598. [1] |
In vivo | METHODS: To detect antitumor activity in vivo, BAY-598 (50 mg/kg once daily) and gemcitabine (100 mg/kg every three days) were administered intraperitoneally to NSG mice bearing SW1990 xenografts for 27 days. RESULTS: The combination of gemcitabine and BAY-598 attenuated the growth of SW1990 xenografts compared to monotherapy. [1] METHODS: To assay anti-tumor activity in vivo, BAY-598 (10-100 mg/kg, PEG 400/water 8:2) was administered orally to BALB/c nude mice bearing KYSE-150 xenografts once daily for three days. RESULTS: BAY-598 was able to inhibit SMYD2 methylation activity in tumor cells in vivo. [2] |
Molecular Weight | 525.34 |
Formula | C22H20Cl2F2N6O3 |
Cas No. | 1906919-67-2 |
Smiles | CCN([C@H]1CN(N=C1c1ccc(Cl)c(Cl)c1)C(\NC#N)=N\c1cccc(OC(F)F)c1)C(=O)CO |
Relative Density. | 1.46 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 125 mg/mL (237.94 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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