IMPDH II/HDAC1-IN-1
IMPDH II/HDAC1-IN-1 (Compound C12) is an orally active, selective dual IMPDH II/HDAC1 inhibitor, with an IC50 of 84.69 nM against hIMPDH II and an IC50 of 81.75 nM against HDAC1. IMPDH II/HDAC1-IN-1 inhibits the proliferation of chronic myeloid leukemia cells. IMPDH II/HDAC1-IN-1 can be used for the research of chronic myeloid leukemia.
For research use only. We do not sell to patients.
- Formula: C22H23N5O3S
- Molecular Weight:437.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HDAC1 81.75 nM (IC50) |
IMPDH2 84.69 nM (IC50) |
IMPDH II/HDAC1-IN-1 (1 μM) potently inhibits IMPDH II, with an IC50 value of 84.69 nM[1].
IMPDH II/HDAC1-IN-1 (1 μM) potently inhibits HDAC1, with an IC50 value of 81.75 nM[1].
IMPDH II/HDAC1-IN-1 (0.0003-20.0 μM; 48 h) potently inhibits the proliferation of K-562 cells, with an IC50 of 305.31 nM[1].
IMPDH II/HDAC1-IN-1 (1 μM; 0-60 min) exhibits moderate in vitro metabolic stability in liver microsomes, with a half-life of 39.2 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K-562 chronic myeloid leukemia cells
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Concentration:0.0003-20.0 μM; 305.31 nM (IC50)
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Incubation Time:48 h
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Result:Inhibited K-562 cell proliferation with an IC50 value of 305.31 nM.
Exhibited superior activity to positive controls MPA (IC50 = 403.23 nM) and SAHA (IC50 = 1165.72 nM).
| Species | Dose | Route | T1/2 | Cmax | AUC0-∞ |
|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | p.o. | 3.05 h | 863 ng/mL | 6258 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) rats[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Reached a peak plasma concentration (Cmax) of 863 ng/mL at 4.67 h (Tmax).
Had an elimination half-life (T1/2) of 3.05 h.
Had an area under the plasma concentration-time curve from time 0 to the last measurable time point (AUC0-t) of 6232 h ng/mL.
Had an area under the curve from time 0 to infinity (AUC0-∞) of 6258 h ng/mL.
Had a mean residence time from time 0 to the last measurable time point (MRT0-t) of 5.78 h.
Had a mean residence time from time 0 to infinity (MRT0-∞) of 5.88 h.
Chemical Information
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Molecular Weight 437.51
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Formula C22H23N5O3S
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SMILES
ONC(CCC1=CC=CC(NC(NC2=CC3=C(C(C4=NCCS4)=CN3C)C=C2)=O)=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IMPDH II/HDAC1-IN-1 Related Classifications
HY-174221 Related Classifications
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