2. Cell Cycle/DNA Damage Epigenetics Cytoskeleton
  3. HDAC Microtubule/Tubulin Histone Methyltransferase
  4. HDAC6-IN-65

HDAC6-IN-65 is a selective HDAC6 inhibitor (IC50 = 0.9 nM) and also exhibits a certain suppressive effect on HDAC3 (IC50 = 39.4 nM). HDAC6-IN-65 can induce the accumulation of α-tubulin (ac-tubulin) and acetylated histone H3 (ac-histone H3, a class I HDAC inhibition marker) in Neuro-2a cells. HDAC6-IN-65 can be used for the study of melanoma.

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HDAC6-IN-65

HDAC6-IN-65 Chemical Structure

CAS No. : 3028442-70-5

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HDAC6-IN-65 Related Antibodies

Top Publications Citing Use of Products

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

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

HDAC6-IN-65 is a selective HDAC6 inhibitor (IC50 = 0.9 nM) and also exhibits a certain suppressive effect on HDAC3 (IC50 = 39.4 nM). HDAC6-IN-65 can induce the accumulation of α-tubulin (ac-tubulin) and acetylated histone H3 (ac-histone H3, a class I HDAC inhibition marker) in Neuro-2a cells. HDAC6-IN-65 can be used for the study of melanoma[1].

IC50 & Target[1]

HDAC6

0.9 nM (IC50)

HDAC3

39.4 nM (IC50)

In Vitro

HDAC6-IN-65 (Compound 14) exhibits significant antiproliferative activity against leukemia cell line (MV4-11, IC50 = 0.57 μM), as well as significant antiproliferative activity against other tumor cells (MM.1S, IC50 = 2.45 μM) (Neuro-2a, IC50 = 6.24 μM) (SH-SY5Y, IC50 = 3.75 μM), and low toxicity to normal cells (HEK-293, IC50 = 6.09 μM) (pNHF, IC50 = 16.24 μM) (MRC9, IC50 = 19.08 μM)[1].
HDAC6-IN-65 (0.05-5 μM) significantly induces the accumulation of α-tubulin (ac-tubulin) in Neuro-2a cells at a concentration of 50 nM (a marker of HDAC6 inhibition), and acetylated histone H3 (ac-histone H3, a class I HDAC inhibition marker) was also increased at a concentration of 1 μM[1].
HDAC6-IN-65 (0.5 μM, 6-72 h), despite its weaker or more transient inhibition of class I HDACs, may exhibit PD effects that persist beyond its systemic exposure in RDES cell line[1].

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

HDAC6-IN-65 Related Antibodies

Western Blot Analysis[1]

Cell Line: RDES cell line
Concentration: 0.5 μM
Incubation Time: 6 h, 12 h, 24 h, 48 h, 72 h
Result: Significantly increased ac-tubulin levels in RDES cells at 6 h, which persist until 48 h, and begin to decline at 72 h. Ac-histone H3 levels increased at 6 and 12 h, but returned to baseline at 24 h.
Parmacokinetics
Species Dose Route Tmax T1/2 Cmax AUClast
Mice 20 mg/kg i.p. 0.25 h 1.66 h 4839 ng/mL 2935 ng·h/mL
In Vivo

HDAC6-IN-65 (Compound 14) (25 mg/kg, i.p., once daily for 14 days, M-F) effectively inhibits tumor growth and activates immune regulation in a mouse SM1 melanoma model, and shows no significant toxicity to mice at the tested concentrations[1].

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

Animal Model: C57BL/6 female mice were injected subcutaneously with 106 in vivo passaged SM1 melanoma cells suspended in 100 μL of PBS[1].
Dosage: 25 mg/kg
Administration: I.p., once daily for 14 days, M-F
Result: The mean tumor growth inhibition rate (TGI) was 56%.
All mice showed normal body weight and organ function, with no signs of toxicity.
Flow cytometry revealed an increase in CD4+ and CD8+ T cells, NK cells, and M1 macrophages, and a decrease in M2 macrophages in the tumor microenvironment.
Molecular Weight

431.89

Formula

C20H18ClN3O4S
CAS No.
SMILES

O=S(N(CC1=CN=CC=C1)CC2=CC=C(C=C2)C(NO)=O)(C3=C(C=CC=C3)Cl)=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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HDAC6-IN-65 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:

HDAC6-IN-653028442-70-5HDACMicrotubule/TubulinHistone MethyltransferaseHistone deacetylasesTO-317SM1 Melanoma ModelHDAC6HDAC3Inhibitorinhibitorinhibit

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