2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. SKLB-23bb

SKLB-23bb 是一种有效的选择性 HDAC6 抑制剂，IC50 为 17 nM，比抑制 HDAC1 (IC50= 422 nM) 和 HDAC8 (IC50=3398 nM) 选择性分别高 25 倍和 200 倍。

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SKLB-23bb Chemical Structure

SKLB-23bb Chemical Structure

CAS No. : 1815580-06-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2420
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1 mg ￥900
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5 mg ￥2200
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10 mg ￥3000
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SKLB-23bb 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

SKLB-23bb is a potent and selective inhibitor for HDAC6 with an IC50 of 17 nM and shows 25-fold and 200-fold selectivity relative to HDAC1 (IC50=422 nM) and HDAC8 (IC50=3398 nM), respectively.

IC50 & Target

IC50: 17 nM (HDAC6), 422 nM (HDAC1), 398 nM (HDAC8)[1]
体外研究
(In Vitro)

SKLB-23bb (Compound 23bb) presents low nanomolar antiproliferative effects against panel of cancer cell lines. The antiproliferative activity is ton human malignant melanoma A375 cells and cervical cancer HeLa cells, SKLB-23bb shows the most potent activities with IC50 values of 50 and 49 nM on A375 and HeLa cells, respectively. The antiproliferative activities against 11 kinds of hematological tumors (myelomaU266, RPMI8226 cells, human leukemia MV4-11, K562 cells, and human B cell lymphoma Ramos cells) or solid tumors (ovarian cancer A2780s, SKOV-3 cells, breast cancer SKBR3 cells, liver cancer HepG2 cells, lung cancer H460, A549 cells, cervical cancer HeLa cells and colon cancer HCT116, HT29 cells) cell lines of SKLB-23bb are evaluated by MTT, and the SAHA and ACY-1215 are as positive control. SKLB-23bb shows significant antiproliferative potential with the IC50 values ranging from 14 to 104 nM in these tumor cell lines[1].

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

SKLB-23bb 相关抗体:
体内研究
(In Vivo)

SKLB-23bb (Compound 23bb) reduces the tumor growth in both the hematological tumor MV4-11 xenograft model and solid tumor HCT116 xenograft model. The significant antitumor activities are observed by intravenous administration of SKLB-23bb at 50 mg/kg on MV4-11 and HCT116 xenograft models. The growth of MV4-11 and HCT116 cancer cell xenografts is suppressed by 55.0% and 76.3% (percent of tumor mass change [TGI] values) after iv administration of SKLB-23bb at 50 mg/kg. The HCT116 xenograft model is also established to investigate the antitumor activity of oral administration of SKLB-23bb. The TGI value of oral administration of SKLB-23bb (25 mg/kg) on HCT116 xenograft model is 60.4%, which is superior to the SAHA group (100 mg/kg, 59.2%). Additionally, the body weight decrease is acceptable and no other adverse effects are observed upon treatment with SKLB-23bb. Low clearance (CL=7.008 L/kg per hour for iv, CL=12.877 L/kg per hour for po) and long terminal half-life (t1/2=7.658 h for iv, t1/2=9.62 h for po) are observed in SKLB-23bb. The oral bioavailability of SKLB-23bb is excellent in rats and the bioavailability is up to 47.0%[1].

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

396.44

Formula

C21H24N4O4
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
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 32 mg/mL (80.72 mM; 超声加热助溶; 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 2.5224 mL 12.6122 mL 25.2245 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.31 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.31 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
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
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: ≥98.0%

COA (285 KB) HNMR (252 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

A375, A2780s, SKBR3, HepG2, HeLa, HCT116, A549, and SKOV-3 cells are cultured in DMEM. RPMI8226, K562, H460, HT29, and Ramos cells are cultured in RPMI-1640 medium. MV4-11 cells are cultured in IMDM. All media contains 10% fetal bovine serum (FBS), 100 units/mL Penicillin, and 100 μg/mL Streptomycin. Cells are incubated at 37 °C in a humidified atmosphere of 5% CO2. Cells in logarithmic phase are seeded into 96-well culture plates at densities of 3000-5000 cells per well and subsequently treated with various concentrations of compounds (e.g., SKLB-23bb;10, 100, 1000, and 10000 nM) for 72 h in final volumes of 200 μL. Upon end point, 20 μL of MTT (5 mg/mL) is added to each well, and the cells are incubated for an additional 1-3 h. After carefully removal of the medium, the precipitates are dissolved in 150 μL of DMSO via mechanically shaking, and then absorbance values at a wavelength of 570 nm are taken on a spectrophotometer. IC50 values are calculated using percentage of growth versus untreated control[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
For the MV4-11 and Ramos xenograft models, MV4-11 and Ramos cells (107 cells in 100 μL of serum-free IMDM) are injected subcutaneously into the right flanks of 5- to 6-week-old female NOD/SCID mice. For the HCT116 xenograft, HCT116 cells (107 cells in 100 μL of serum-free DMEM) are injected subcutaneously into the right flanks of 5- to 6-week-old female Balb/c nude mice. When the size of the formed xenografts reach 100-150 mm3, the mice are randomly divided (6 mice per group in MV4-11 model, 8 mice per group in Ramos model, and 7 mice per group in HCT116 model) into control group and treated groups. The mice in the experimental groups receive intravenous (iv) injection (50 mg/kg) or oral administration (25 mg/kg) of SKLB-23bb every 2 days. The mice in the vehicle group receive iv injection or oral administration of equal amount of physiological saline containing 5% ethanol and 5% Cremophor EL. Those in the SAHA or LBH-589 or ACY-1215 groups (positive controls) receive ip injection (50 mg/kg for SAHA and 10 mg/kg for LBH-589, dissolved in physiological saline containing 10% DMSO and 45% PEG400 to a concentration of 10 mg/mL) or oral administration (100 mg/kg for SAHA and 40 mg/kg for ACY-1215, dissolved in the same way described above) every 2 days. Tumor burden is measured every 2 days by a caliper. Tumor volume (TV) is calculated. The day that treatment started is defined as day 0. At the end of the experiment, mice are sacrificed and tumors are collected and weighed[1].
Rats[1]
SKLB-23bb is administered to SD rats ntravenously (iv) at 12 mg/kg body weight and orally at 12 mg/kg body weight. Blood samples are taken, and the plasma is analyzed for concentration of SKLB-23bb using an LC-MS/MS system[1].

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

SKLB-23bb 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5224 mL 12.6122 mL 25.2245 mL 63.0612 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 mL 12.6122 mL
10 mM 0.2522 mL 1.2612 mL 2.5224 mL 6.3061 mL
15 mM 0.1682 mL 0.8408 mL 1.6816 mL 4.2041 mL
20 mM 0.1261 mL 0.6306 mL 1.2612 mL 3.1531 mL
25 mM 0.1009 mL 0.5045 mL 1.0090 mL 2.5224 mL
30 mM 0.0841 mL 0.4204 mL 0.8408 mL 2.1020 mL
40 mM 0.0631 mL 0.3153 mL 0.6306 mL 1.5765 mL
50 mM 0.0504 mL 0.2522 mL 0.5045 mL 1.2612 mL
60 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0510 mL
80 mM 0.0315 mL 0.1577 mL 0.3153 mL 0.7883 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:

SKLB-23bb1815580-06-3HDACHistone deacetylasesInhibitorinhibitorinhibit

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