2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. HDAC6-IN-13

HDAC6-IN-13 (Compound 35m) 是一种强效、高选择性、具有口服活性的 HDAC6 抑制剂，其 IC50 为 0.019 μM。 HDAC6-IN-13 也抑制 HDAC1、HDAC2 和 HDAC3，IC50 分别为 1.53、2.06 和 1.03 μM。 HDAC6-IN-13 具有明显的血脑屏障通透性和抗炎活性。

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HDAC6-IN-13 Chemical Structure

HDAC6-IN-13 Chemical Structure

CAS No. : 2837128-41-1

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5 mg ￥4500
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Customer Review

HDAC6-IN-13 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

HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity[1].

IC50 & Target[1]

HDAC6

0.019 μM (IC50)

HDAC3

1.03 μM (IC50)

HDAC1

1.53 μM (IC50)

HDAC2

2.06 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
J774.A1 IC50
2.61 μM
Compound: 35m
Antiinflammatory activity against LPS primed mouse J774.A1 cells assessed suppression of LPS/ATP induced IL-beta release preincubated for 30 mins followed by ATP stimulation measured after 30 mins by ELISA
Antiinflammatory activity against LPS primed mouse J774.A1 cells assessed suppression of LPS/ATP induced IL-beta release preincubated for 30 mins followed by ATP stimulation measured after 30 mins by ELISA
[PMID: 36073117]
体外研究
(In Vitro)

HDAC6-IN-13 (Compound 35m) (0.1-1 μM; 24 h) is highly selective toward HDAC6 versus class I HDACs[1].
HDAC6-IN-13 is a slow-on and slow-off tight-binding HDAC6 inhibitor, while exhibits fast-on properties for HDAC1, 2, and 3[1].
HDAC6-IN-13 (5-20 μM; 8 h) shows anti-inflammatory activity in vitro[1].

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

HDAC6-IN-13 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4−11 and J774A.1
Concentration: 0.1, 0.2, 0.5 and 1 μM
Incubation Time: 24 h
Result: Concentration-related accumulation of acetylated tubulin (Ac-Tubulin) was observed, while upregulation of acetylated histone H3 (AcHH3) and acetylated histone H4 (AcHH4) was not apparent even at the concentration of 1 μM.

Western Blot Analysis[1]

Cell Line: J774A.1 cells
Concentration: 5, 10 and 20 μM
Incubation Time: 8 h
Result: Inhibited the cleavage of pro-caspase 1 to p20 in a dose-dependent manner, inhibited the interaction between HDAC6 and dynein.
体内研究
(In Vivo)

HDAC6-IN-13 (Compound 35m) (20 mg/kg; p.o. and i.p.; once) displays a remarkable inhibition in LPS-induced inflammation in mice[1].
HDAC6-IN-13 (20 mg/kg; p.o.; once) shows very high oral bioavailability (F% = 93.4%) and significant BBB permeability in mice[1].

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

Animal Model: Male C57BL/6 WT mice, LPS-induced endotoxic shock model[1]
Dosage: 20 mg/kg
Administration: PO and IP, immediately after the LPS injection
Result: Significantly decreased the serum IL-1β levels in LPS-induced mice via both ip and po administration.
Animal Model: Male CD-1 mice[1]
Dosage: 5 mg/kg or 20 mg/kg
Administration: IV (5 mg/kg) or PO (20 mg/kg) (Pharmacokinetic Study)
Result: Pharmacokinetics Characterization of HDAC6-IN-13 (Compound 35m) with iv and Oral Administrationa[1]
PK parameters HDAC6-IN-13 HDAC6-IN-13
administered dose (mg/kg) iv at 5 mg/kg oral at 20 mg/kg
Cmax (ng/mL) 4604 ± 551 5570 ± 551
t1/2 (h) 7.95 ± 0.370 6.80 ± 0.145
AUC0−inf (ng•h/mL) 2755 ± 395 10292 ± 1385
F% n/a 93.4 ± 12.6

aHDAC6-IN-13 was administrated via iv and po (n = 3). The blood sample was collected at different time points after dosing, and the plasma concentration of HDAC6-IN-13 was determined via LC-MS/MS. The area under the plasma concentration versus time curve (AUC) was calculated using the linear trapezoidal method. The pharmacokinetic parameters were obtained using the noncompartmental method. Data are shown as mean ± SD.
分子量

370.45

Formula

C23H22N4O
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (337.43 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6994 mL 13.4971 mL 26.9942 mL
5 mM 0.5399 mL 2.6994 mL 5.3988 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

HDAC6-IN-13 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6994 mL 13.4971 mL 26.9942 mL 67.4855 mL
5 mM 0.5399 mL 2.6994 mL 5.3988 mL 13.4971 mL
10 mM 0.2699 mL 1.3497 mL 2.6994 mL 6.7485 mL
15 mM 0.1800 mL 0.8998 mL 1.7996 mL 4.4990 mL
20 mM 0.1350 mL 0.6749 mL 1.3497 mL 3.3743 mL
25 mM 0.1080 mL 0.5399 mL 1.0798 mL 2.6994 mL
30 mM 0.0900 mL 0.4499 mL 0.8998 mL 2.2495 mL
40 mM 0.0675 mL 0.3374 mL 0.6749 mL 1.6871 mL
50 mM 0.0540 mL 0.2699 mL 0.5399 mL 1.3497 mL
60 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
80 mM 0.0337 mL 0.1687 mL 0.3374 mL 0.8436 mL
100 mM 0.0270 mL 0.1350 mL 0.2699 mL 0.6749 mL
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-132837128-41-1HDACHistone deacetylasesAlzheimer’s diseaseanti-inflammatory activityorally activeBBB permeabilityInhibitorinhibitorinhibit

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