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IOX1 is a histone demethylase JMJD inhibitor (IC50 values are 0.12, 0.17, 0.2, 0.3, 0.6 and 1 μM for JMJD3, JMJD1A, JMJD2A, JMJD2E, JMJD2C and UTX respectively). IOX1 inhibits JMJD2A-mediated H3K9me3 demethylation in HeLa cells. IOX1 also inhibits ALKBH5.
| Molecular Weight | 189.17 |
| Formula | C10H7NO3 |
| CAS Number | 5852-78-8 |
| Solubility (25°C) | DMSO: 15 mg/mL (Need ultrasonic and warming) |
| 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.
| Related Histone demethylases Products |
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| Pulrodemstat
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine-specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. |
| TAK-418
TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. It is an orally administered CNS-permeable clinical candidate for the study of neurodevelopmental disorders, such as autism spectrum disorders. |
| L-2-Hydroxyglutaric acid disodium
L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. L-2-Hydroxyglutaric acid disodium is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively. |
| PBIT
PBIT is a JARID1 (Jumonji AT-Rich Interactive Domain 1) inhibitor with IC50 values of 3, 4.9 and 6 μM for JARID1B, 1A and 1C, respectively. It can increase trimethylation of H3K4 in HeLa cells and block the proliferation of tumor cells expressing high levels of JARID1B. |
| Seclidemstat mesylate
Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). |
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