2. Metabolic Enzyme/Protease Epigenetics Cell Cycle/DNA Damage
  3. IMPDH HDAC
  4. 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.

IMPDH II/HDAC1-IN-1

IMPDH II/HDAC1-IN-1 Chemical Structure

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IMPDH II/HDAC1-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

HDAC1

81.75 nM (IC50)

IMPDH2

84.69 nM (IC50)

In Vitro

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.

IMPDH II/HDAC1-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: K-562 chronic myeloid leukemia cells
Concentration: 0.0003-20.0 μM; 305.31 nM (IC50)
Incubation Time: 48 h
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).
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-∞
Rat[1] 10 mg/kg p.o. 3.05 h 863 ng/mL 6258 ng·h/mL
In Vivo

IMPDH II/HDAC1-IN-1 (C12) (10 mg/kg; p.o.; single dose) exhibits acceptable in vivo pharmacokinetic properties in SD rats following a single 10 mg/kg oral dose, with a peak plasma concentration of 863 ng/mL, elimination half-life of 3.05 h, and systemic exposure of 6258 h ng/mL[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (SD) rats[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

437.51

Formula

C22H23N5O3S
SMILES

ONC(CCC1=CC=CC(NC(NC2=CC3=C(C(C4=NCCS4)=CN3C)C=C2)=O)=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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IMPDH II/HDAC1-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IMPDH II/HDAC1-IN-1IMPDHHDACInosine-5’-monophosphate dehydrogenaseHistone deacetylaseszinc ionsHis178His93HDAC1HDAC11HDAC4hIMPDH IITyr204hydroxamic acid moietychronic myeloid leukemiaInhibitorinhibitorinhibit

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