2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. HDAC8-IN-16

HDAC8-IN-16 is a selective histone deacetylase 8 (HDAC8) inhibitor with an IC50 of 0.16 μM. HDAC8-IN-16 induces cell apoptosis, triggers G2/M phase cell cycle arrest, and moderately inhibits cancer cell proliferation. HDAC8-IN-16 is applicable to relevant research on colorectal cancer.

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HDAC8-IN-16

HDAC8-IN-16 Chemical Structure

CAS No. : 2464465-06-1

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HDAC8-IN-16 Related Antibodies

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Description

HDAC8-IN-16 is a selective histone deacetylase 8 (HDAC8) inhibitor with an IC50 of 0.16 μM. HDAC8-IN-16 induces cell apoptosis, triggers G2/M phase cell cycle arrest, and moderately inhibits cancer cell proliferation. HDAC8-IN-16 is applicable to relevant research on colorectal cancer[1].

IC50 & Target[1]

HDAC8

0.16 μM (IC50)

In Vitro

HDAC8-IN-16 (Compound 16) (48 h) exhibits moderate antiproliferative activity against Jurkat, MOLT-4 and HCT116 tumor cells, with the strongest activity against HCT116 cells (IC50 = 16.12 μM), while it shows only weak or no activity against K562, HL-60 and HeLa cells[1].
HDAC8-IN-16 (5-20 μM; 48 h) significantly increases the acetylation level of SMC3, a specific substrate of HDAC8, in HCT116 cells, confirming that it inhibits HDAC8 at the cellular level[1].
HDAC8-IN-16 (5-20 μM; 48 h) induces dose-dependent apoptosis in HCT116 cells[1].
HDAC8-IN-16 (5-20 μM; 48 h) arrests HCT116 cells at the G2/M phase of the cell cycle in a dose-dependent manner[1].

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

HDAC8-IN-16 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 48 h
Result: Had a marginal effect on Ac-SMC3 levels at 5 μM and 10 μM.
Induced a significant, noticeable accumulation of Ac-SMC3 at 20 μM.
Had no significant effect on Ac-α-tubulin or histone H3 acetylation levels.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 48 h (treatment); 15 min (staining incubation at room temperature)
Result: Increased early apoptosis from 1.87% to 2.81% and late apoptosis from 0.90% to 3.12% at 5 μM.
Increased early apoptosis to 17.37% and late apoptosis to 7.53% at 10 μM.
Increased early apoptosis to 17.37% and late apoptosis to 25.57% at 20 μM, showing a dose-dependent increase in apoptotic cells.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 48 h (treatment); overnight (fixation at 4 °C); 30 min (staining incubation at room temperature)
Result: Decreased G0/G1 phase from 67.23% to 57.84%, increased S phase from 16.87% to 19.01%, and increased G2/M phase from 15.90% to 23.15% at 5 μM.
Decreased G0/G1 phase to 40.67%, increased S phase to 27.13%, and increased G2/M phase to 32.20% at 10 μM.
Decreased G0/G1 phase to 27.62%, increased S phase to 27.02%, and increased G2/M phase to 45.36% at 20 μM, showing a pronounced G2/M phase arrest.
Molecular Weight

380.44

Formula

C21H24N4O3
CAS No.
SMILES

O=C(N1CCC(CC1)[C@H](CO)O)C2=NN(C3=C2C=CC=N3)CC4=CC=CC=C4
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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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HDAC8-IN-16 Related Classifications

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  • 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:

HDAC8-IN-162464465-06-1HDACApoptosisHistone deacetylasescolorectal cancerSMC3apoptosishistone deacetylase 8G2/M phase cell cycle arrestJurkatMOLT-4HDAC1HDAC8HCT116Inhibitorinhibitorinhibit

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