SGI-110 (S-110) is a stable and potent inhibitor for DNA methylation, inhibits DNMT1 when SGI-110 is activated by phosphorylation and incorporated into DNA.
| Molecular Weight | 579.39 |
| Formula | C18H23N9O10P.Na |
| CAS Number | 929904-85-8 |
| Form | Solid |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Caner Saygin, et al. Current and emerging strategies for management of myelodysplastic syndromes
| Related DNA Methyltransferase Products |
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| (S)-GSK-3685032
(S)-GSK-3685032 is the inactive isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition. |
| (R)-GSK-3685032
(R)-GSK-3685032 is the R-isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition. |
| DNMT-IN-1
DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM. |
| DNMT2-IN-1
DNMT2-IN-1 is a potent and selective DNMT2 (DNA methyltransferase 2) inhibitor with an IC50 value of 1.2 μM, and has the potential for mental and metabolic disorders or cancer research. |
| Guadecitabine
Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS). |
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