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

TNI-97 是一种具有选择性且口服活性的 HDAC6 抑制剂，其 IC50 值为 0.2 nM。TNI-97 显著抑制三阴性乳腺癌 (TNBC) 细胞系 MDA-MB-453 的生长和集落形成能力。TNI-97 在 MDA-MB-453 细胞中诱导泛凋亡包括凋亡 (apoptosis)、坏死性凋亡 (necroptosis) 和焦亡 (pyroptosis)。TNI-97 在携带 MDA-MB-453 异种移植瘤或小鼠源性 TNBC 细胞同种异体移植瘤的小鼠模型中显示出抗肿瘤活性。TNI-97 可用于三阴性乳腺癌的研究。

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TNI-97

TNI-97 Chemical Structure

CAS No. : 2790425-52-2

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TNI-97 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

TNI-97 在 MDA-MB-453 细胞和 MDA-MB-468 细胞中显示出抗肿瘤活性，GI50值分别为 0.2 μM 和 5.4 μM[1]。
TNI-97 (1 μM, 24 h) 在较低浓度下显著诱导 MDA-MB-453 细胞中 α-tubulin 乙酰化，效果优于 Ricolinostat (ACY-1215) (HY-16026)，且不诱导组蛋白 H3 乙酰化[1]。
TNI-97 (1-2 μM, 14 days) 以剂量依赖性方式抑制 MDA-MB-453 细胞的集落形成[1]。
TNI-97 (2.5-5 μM, 48 h) 在 MDA-MB-453 细胞中诱导凋亡、坏死性凋亡和焦亡[1]。

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

TNI-97 相关抗体:

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.
体内研究
(In Vivo)

TNI-97 (20-40 mg/kg，口服，5 天给药/停药 2 天，持续 5 周) 在携带 MDA-MB-453 异种移植瘤的 NSIG 小鼠中表现出剂量依赖性的肿瘤生长抑制作用[1]。
TNI-97 (40 mg/kg，口服，5 天给药/停药 2 天，持续 2 周) 在与 Paclitaxel (HY-B0015) 联用时可显著降低携带 TNBC 细胞同种异体移植瘤的 BALB/c 小鼠中的肿瘤重量和肿瘤体积[1]。

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.
分子量

416.36

Formula

C19H15F3N6O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TNI-97 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

TNI-972790425-52-2TNI97TNI 97HDACApoptosisPyroptosisNecroptosisHistone deacetylasespyroptosisapoptosistriple-negative breast cancerMDA-MB-453 cellsInhibitorinhibitorinhibit

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目录号：
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