2. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  3. HDAC SHMT Apoptosis Reactive Oxygen Species (ROS) Ferroptosis
  4. HDAC11-IN-5

HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC50 of 0.021 μM. HDAC11-IN-5 increases fatty acylation levels of substrate SHMT2 in AML cells. HDAC11-IN-5 induces apoptosis, G1 phase cell cycle arrest, ferroptosis, ROS production and terminal myeloid differentiation in AML cells. HDAC11-IN-5 demonstrates anti-tumor potency in an MLL-AF9-induced mouse AML model. HDAC11-IN-5 can be used for the research of cancer, such as acute myeloid leukemia.

For research use only. We do not sell to patients.

HDAC11-IN-5

HDAC11-IN-5 Chemical Structure

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HDAC11-IN-5 Related Antibodies

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC50 of 0.021 μM. HDAC11-IN-5 increases fatty acylation levels of substrate SHMT2 in AML cells. HDAC11-IN-5 induces apoptosis, G1 phase cell cycle arrest, ferroptosis, ROS production and terminal myeloid differentiation in AML cells. HDAC11-IN-5 demonstrates anti-tumor potency in an MLL-AF9-induced mouse AML model. HDAC11-IN-5 can be used for the research of cancer, such as acute myeloid leukemia[1].

IC50 & Target[1]

HDAC11

0.021 μM (IC50)

SHMT2

 

In Vitro

HDAC11-IN-5 (Compound 25) potently inhibits purified HDAC11 protein with an IC50 of 0.021 ± 0.005 μM, and shows no significant inhibition of HDAC1, HDAC6, HDAC7, or HDAC8 at concentrations up to 10 μM[1].
HDAC11-IN-5 (96 h) potently inhibits proliferation of U937, OCI-AML2, THP-1, and MOLM13 AML cell lines with IC50 values of 6.3 μM, 5.7 μM, 5.4 μM, and 6.7 μM, respectively[1].
HDAC11-IN-5 (10-20 μM; 6 h) selectively inhibits intracellular HDAC11 in U937 AML cells, as shown by increased SHMT2 fatty acylation at 10 μM for 6 h and no significant changes in histone H3 or α-tubulin acetylation at 20 μM for 6 h[1].
HDAC11-IN-5 (8 μM; 48 h) strongly induces apoptosis in U937 and OCI-AML2 AML cells[1].
HDAC11-IN-5 (8 μM; 48 h) induces G1-phase cell cycle arrest in U937 AML cells[1].
HDAC11-IN-5 (8 μM; 48 h) promotes myeloid differentiation of U937 AML cells, as shown by increased CD14 and CD11b expression[1].
HDAC11-IN-5 (8 μM; 48 h) induces ferroptosis in U937 AML cells, as shown by increased lipid peroxidation, cellular ROS, and intracellular Fe2+ levels[1].
HDAC11-IN-5 (5-20 μM; 96 h) exhibits strong synergistic antiproliferative activity with ivosidenib in U937, OCI-AML2, and MLL-AF9 mouse AML cells[1].

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

HDAC11-IN-5 Related Antibodies

Western Blot Analysis[1]

Cell Line: U937 AML cells
Concentration: 10 μM (SHMT2 fatty acylation analysis); 20 μM (histone H3 and α-tubulin acetylation analysis)
Incubation Time: 6 h
Result: Significantly increased fatty acylation levels of SHMT2 (a specific HDAC11 substrate) at 10 μM for 6 h.
Had negligible effects on acetylation levels of histone H3 (a class I HDAC substrate) and α-tubulin (an HDAC6 substrate) at 20 μM for 6 h.

Apoptosis Analysis[1]

Cell Line: U937, OCI-AML2 AML cell lines
Concentration: 8 μM
Incubation Time: 48 h
Result: Significantly induced apoptosis in both U937 and OCI-AML2 cells.

Cell Differentiation Assay[1]

Cell Line: U937 AML cells
Concentration: 8 μM
Incubation Time: 48 h
Result: Significantly increased expression of the myeloid differentiation markers CD14 and CD11b in U937 cells, with a stronger effect than FT895.
Parmacokinetics
Species Dose Route T1/2 AUC0-∞ Vss CL Tmax Cmax F
Mice[1] 5 mg/kg i.v. 3.74 h 613 ng·h/mL 14.87 L/kg 136 mL/min/kg / / /
Mice[1] 50 mg/kg p.o. 2.39 h 1273 ng·h/mL / / 0.25 h 812 ng/mL 20.8 %
In Vivo

HDAC11-IN-5 (Compound 25) (50 mg/kg; i.g.; once daily; 14 days) reduces peripheral blood leukemic cell burden and significantly extends survival in an MLL-AF9-induced AML mouse model, with enhanced efficacy when combined with Ivosidenib (HY-18767)[1].

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

Animal Model: C57BL/6 (6-week-old female, 20-22 g, tail vein injection of 1×105 MLL-AF9-GFP+ leukemic cells)[1]
Dosage: 50 mg/kg
Administration: I.g.,; once daily; 14 days
Result: Reduced the percentage of GFP+ leukemic cells in peripheral blood.
Significantly extended the survival of AML mice compared to vehicle control.
Reduced the percentage of GFP+ leukemic cells when combined with ivosidenib, with greater survival extension than either agent alone.
Caused no significant body weight loss prior to the moribund stage.
Molecular Weight

529.38

Formula

C24H25Cl2F3N4O2
SMILES

O=C(C1=CC=CC2=C1C=C(C#CC3=CC=CC(C(F)(F)F)=C3)N2CCN4CCNCC4)NO.Cl.Cl
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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HDAC11-IN-5 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:

HDAC11-IN-5HDACSHMTApoptosisReactive Oxygen Species (ROS)FerroptosisHistone deacetylasesSerine hydroxymethyltransferaseCD14CD11bG1 phase cell cycle arrestHDAC11terminal myeloid differentiationapoptosisMLL-AF9-induced mouse AML modelferroptosisSHMT2AML cellsInhibitorinhibitorinhibit

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