2. Cell Cycle/DNA Damage Epigenetics Cytoskeleton Apoptosis
  3. HDAC Microtubule/Tubulin Caspase Apoptosis
  4. HDAC1-IN-5

HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice.

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HDAC1-IN-5 Chemical Structure

HDAC1-IN-5 Chemical Structure

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HDAC1-IN-5 Related Antibodies

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1 Publications Citing Use of MCE HDAC1-IN-5

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

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice[1].

IC50 & Target[1]

HDAC1

15 nM (IC50)

HDAC6

20 nM (IC50)

In Vitro

HDAC1-IN-5 (compound 4j) (0-50 μM; 48 h) exhibits strong inhibitory effects on HCT116, HeLa, HepG2, MC38, K562 and HEL[1].
HDAC1-IN-5 (0.16-1.5 μM; 48 h) induces apoptosis in a dose-dependent manner[1].
HDAC1-IN-5 (0.17-1.5 μM; 24 h or 48 h) induces downregulation of SPT16 and SSRP-1, induces the cleavage of caspase-3, and increases the expression of Acetyl-Histone H3 and Acetyl-α-tubulin[1].

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

HDAC1-IN-5 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCT116, HeLa, HepG2, MC38, K562 and HEL
Concentration: 0-50 μM
Incubation Time: 48 h
Result: Showed strong inhibitory effects on HCT116, HeLa, HepG2, MC38, K562 and HEL with IC50s of 0.47 μM, 0.78 μM, 1.4 μM, 0.43 μM, 0.91 μM and 0.28 μM, respectively.

Apoptosis Analysis[1]

Cell Line: HCT116
Concentration: 0.16 μM, 0.5 μM and 1.5 μM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner, and induced 38.5% at the concentration of 1.5 μM (both early and late apoptotic cells).

Western Blot Analysis[1]

Cell Line: HCT116 and MC38
Concentration: 0.17 μM, 0.5 μM and 1.5 μM
Incubation Time: 24 h or 48 h
Result: Induced downregulation of SPT16 and SSRP-1 in HCT116.
Induced the cleavage of caspase-3 in HCT116 and MC38.
Increased the expression of HDAC1, 2, 6 substrate Acetyl-Histone H3 and Acetyl-α-tubulin with a dose-dependent manner.
In Vivo

HDAC1-IN-5 (50 and 100 mg/kg; IP; every two days; for 16 days) significantly decreases the tumor volume and weight in MC38 xenograft mice[1].

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

Animal Model: C57BL/6 mice (6-10 weeks; 2×106 MC38 cells were injected subcutaneously into the right flank regions)[1]
Dosage: 50 and 100 mg/kg
Administration: IP; every two days; for 16 days
Result: Significantly decreased the tumor volume and weight with tumor growth inhibition (TGI) of 66% at 50 mg/kg.
Molecular Weight

367.46

Formula

C20H21N3O2S
SMILES

ONC(CCCCCC1=CC=CC(C2=NN=C(C3=CC=CC=C3)S2)=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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HDAC1-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:

HDAC1-IN-5HDACMicrotubule/TubulinCaspaseApoptosisHistone deacetylasesanticancerHCT116MC38tumor growthC57BL/6 miceInhibitorinhibitorinhibit

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