1. Cell Cycle/DNA Damage Epigenetics Apoptosis Immunology/Inflammation
  2. HDAC Apoptosis Pyroptosis Necroptosis
  3. TNI-97

TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC50 of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer.

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

TNI-97 Chemical Structure

TNI-97 Chemical Structure

CAS No. : 2790425-52-2

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Description

TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC50 of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer[1].

IC50 & Target

HDAC6

0.2 nM (IC50)

HDAC1

2890 nM (IC50)

HDAC2

1306 nM (IC50)

HDAC3

3177 nM (IC50)

HDAC8

4130 nM (IC50)

HDAC4

>5000 nM (IC50)

HDAC5

>5000 nM (IC50)

HDAC7

>5000 nM (IC50)

HDAC9

>5000 nM (IC50)

HDAC11

>5000 nM (IC50)

HDAC10

3162 nM (IC50)

In Vitro

TNI-97 demonstrates antitumor activity with GI50 values of 0.8 μM in MDA-MB-453 cells and 5.4 μM in MDA-MB-468 cells[1].
TNI-97 (1 μM, 24 h) significantly induces α-tubulin acetylation than does Ricolinostat (ACY-1215) (HY-16026) under lower concentrations and does not induce histone H3 acetylation in MDA-MB-453 cells[1].
TNI-97 (1-2 μM, 14 days) dose-dependently inhibits the MDA-MB-453 colony formation[1].
TNI-97 (2.5-5 μM, 48 h) induces apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells[1].

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

Apoptosis Analysis[1]

Cell Line: MDA-MB-453 cells
Concentration: 2.5, 5 μM
Incubation Time: 48 h
Result: Induced apoptosis in MDA-MB-453 cells in a concentration-dependent manner.

Immunofluorescence[1]

Cell Line: MDA-MB-453 cells
Concentration: 5 μM
Incubation Time: 48 h
Result: Increased proportion of YPI/PI dual-positive cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-453 cells
Concentration: 1, 5 μM
Incubation Time: 24 h
Result: Elevated the expression of cleaved forms of executive caspase 3and caspase 7.
Upregulated cleaved forms of GSDMD and GSDME.
In Vivo

TNI-97 (20-40 mg/kg, p.o., 5 on/2 off, 5 weeks) exhibits a dose-dependent inhibition of tumor growth in NSIG mice carrying the MDA-MB-453 xenograft[1].
TNI-97 (40 mg/kg, p.o., 5 on/2 off, 2 weeks) exhibits significant reductions in both tumor weight and tumor size in BALB/c mice carrying murine-derived TNBC cell allografts when combined with Paclitaxel (HY-B0015)[1].

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

Animal Model: NOD-PrkdcscidlL2rgtm1 (NSIG) female mice (6-8 weeks) carrying the MDA-MB-453 xenograft(1 × 107) [1]
Dosage: 20, 40 mg/kg
Administration: p.o. 5 on/2 off for 2 weeks
Result: Exhibited a dose-dependent inhibition of tumor growth, achieving tumor growth inhibition (TGI) rates of 91 and 54% at doses of 40 and 20 mg/kg, respectively.
Induced pANoptosis in tumor tissue.
Upregulated cleaved-caspase 3, cleavedGSDMD, and phosphorylated MLKL expression.
Had no impact on the counts and proportions of white blood cells, red blood cells, and platelets.
Showed no significant morphological abnormalities.
Animal Model: BALB/c mice (6-8 weeks) carrying murine-derived TNBC cell allografts (1 × 106
Dosage: 40 mg/kg
Administration: p.o. 5 on/2 off for 2 weeks
Result: Exhibited significant reductionsin both tumor weight and tumorsize of 4T1 allografts (TGI = 60%).
Showed no significant alteration in body weight.
Molecular Weight

416.36

Formula

C19H15F3N6O2

CAS No.
SMILES

CN1N=NC2=C1C=CC(C3=NN(CC4=CC=C(C=C4)C(NO)=O)C(C(F)(F)F)=C3)=C2

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

Purity & Documentation
References
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TNI-97
Cat. No.:
HY-175030
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