1. Cell Cycle/DNA Damage Epigenetics Apoptosis Cytoskeleton
  2. HDAC Apoptosis Microtubule/Tubulin
  3. NN-429

NN-429 is a selective HDAC6 inhibitor. NN-429 induces apoptosis, increases the acetylation level of α-tubulin, and exhibits cytotoxicity against cancer cells. NN-429 is applicable to research related to acute myeloid leukemia, multiple myeloma and lymphoma.

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NN-429

NN-429 Chemical Structure

CAS No. : 2490284-32-5

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Description

NN-429 is a selective HDAC6 inhibitor. NN-429 induces apoptosis, increases the acetylation level of α-tubulin, and exhibits cytotoxicity against cancer cells. NN-429 is applicable to research related to acute myeloid leukemia, multiple myeloma and lymphoma[1][2].

IC50 & Target[2]

hHDAC6

3.2 μM (IC50)

Zebrafish HDAC6

28.8 μM (IC50)

In Vitro

NN-429 (I-50) potently inhibits purified human HDAC6 with an IC50 of 0.017 μM[1].
NN-429 inhibits the viability of MV-4-11 acute myeloid leukemia cells with an IC50 of 1.6 μM; it also inhibits the viability of MM.1S multiple myeloma cells with an IC50 of 1.2 μM, but shows no significant toxicity to MRC9 healthy lung fibroblasts[1].
NN-429 (6 h) selectively inhibits HDAC6 activity in MV-4-11 acute myeloid leukemia cells and MM.1S multiple myeloma cells[1].
NN-429 induces apoptosis in MV-4-11 acute myeloid leukemia cells in a concentration-dependent manner[1].
NN-429 potently and selectively inhibits purified human HDAC6 with an IC50 of 3.2 nM[2].
NN-429 (28.8 nM) binds to the catalytic domain 2 of recombinant zebrafish HDAC6, with an IC50 of 28.8 nM[2].
NN-429 (0-5 μM; 6 h) selectively binds to HDAC6 in MM.1S multiple myeloma cells and MV4-11 acute myeloid leukemia cells, induces dose-dependent α-tubulin acetylation, and exhibits extremely weak off-target acetylation of histone H3[2].
NN-429 (72 h) exhibits selective cytotoxicity against human γδ T-cell lymphoma (DERL-2, DERL-7) and NK/T-cell lymphoma (MTA, YT) cell lines, with IC50 values ranging from 0.72 to 2.32 μM, whereas it shows only extremely low activity against cutaneous T-cell lymphoma cells (Myla, IC50 >50 μM)[2].
NN-429 (0.1-5 μM; 18 h) induces dose-dependent early apoptosis in DERL-2 γδ T-NHL cells[2].
NN-429 (0.5-5 μM; 24 h) selectively binds to HDAC6 in YT NKTCL cells, induces dose-dependent α-tubulin acetylation, and exhibits extremely weak off-target acetylation of histone H3[2].

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

Western Blot Analysis[2]

Cell Line: MM.1S multiple myeloma cells, MV4-11 acute myeloid leukemia cells
Concentration: 0.1-5 μM (MM.1S cells); 0.25-1 μM (MV4-11 cells)
Incubation Time: 6 h (MM.1S cells); 6 h (MV4-11 cells)
Result: Induced a dose-dependent increase in α-tubulin acetylation starting at 0.1 μM in MM.1S cells.
Caused minimal off-target acetylation of histone H3 only at 5 μM in MM.1S cells.
Induced strong dose-dependent α-tubulin acetylation with minimal histone H3 acetylation across all tested concentrations in MV4-11 cells.

Apoptosis Analysis[2]

Cell Line: DERL-2 γδ T-NHL cells
Concentration: 0.1-5 μM
Incubation Time: 18 h
Result: Induced dose-dependent early-stage apoptosis in DERL-2 cells.
Caused 15% of cells to enter early-stage apoptosis (Annexin V+/PI−) after treatment with 0.1 μM.
Caused 56% of cells to enter early-stage apoptosis after treatment with 5 μM.

Western Blot Analysis[2]

Cell Line: YT NKTCL cells
Concentration: 0.5-5 μM
Incubation Time: 24 h
Result: Induced dose-dependent α-tubulin acetylation in YT cells, with minimal histone H3 acetylation.
Parmacokinetics
Species Dose Route T1/2 Cmax AUClast AUCinf
Mice[2] 50 mg/kg i.p. 3.53 h 3193 ng/mL 9856 ng·h/mL 9923 ng·h/mL
Molecular Weight

438.37

Formula

C17H15F5N2O4S

CAS No.
SMILES

O=C(C1=CC=C(CN(S(=O)(C2=CC(F)=C(C(F)=C2F)F)=O)C(C)C)C(F)=C1)NO

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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.

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NN-429
Cat. No.:
HY-182649
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