SKLB-23bb
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 1815580-06-3
- Formula: C21H24N4O4
- Molecular Weight:396.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
IC50: 17 nM (HDAC6), 422 nM (HDAC1), 398 nM (HDAC8)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
46 nM
Compound: 23bb
|
Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| A2780S | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human A2780S cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human A2780S cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| A-375 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human A-375 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human A-375 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| A-375 | IC50 |
45 nM
Compound: 23bb
|
Antiproliferative activity against human A375 cells after 72 hrs by MTT assay
Antiproliferative activity against human A375 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| A549 | IC50 |
104 nM
Compound: 23bb
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| A549 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| HBL1 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| HCT-116 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| HCT-116 | IC50 |
35 nM
Compound: 23bb
|
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| HeLa | EC50 |
1741 nM
Compound: 23bb
|
Induction of histone H3 acetylation in human HeLa cells incubated for 6 hrs by cytoblot assay
Induction of histone H3 acetylation in human HeLa cells incubated for 6 hrs by cytoblot assay
|
[PMID: 26443078] |
| HeLa | EC50 |
58.9 nM
Compound: 23bb
|
Inhibition of HDAC6 in human HeLa cells assessed as induction of tubulin acetylation incubated for 6 hrs by cytoblot assay
Inhibition of HDAC6 in human HeLa cells assessed as induction of tubulin acetylation incubated for 6 hrs by cytoblot assay
|
[PMID: 26443078] |
| HeLa | IC50 |
49 nM
Compound: 23bb
|
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| HepG2 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| HepG2 | IC50 |
41 nM
Compound: 23bb
|
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| HT-29 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| HT-29 | IC50 |
72 nM
Compound: 23bb
|
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| JeKo-1 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human JeKo-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human JeKo-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| K562 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| K562 | IC50 |
63 nM
Compound: 23bb
|
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| MCF7 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| MDA-MB-231 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| MM1.S | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| MV4-11 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| MV4-11 | IC50 |
60 nM
Compound: 23bb
|
Cytotoxicity against human MV4-11 cells after 72 hrs by MTT assay
Cytotoxicity against human MV4-11 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| NCI-H460 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| NCI-H460 | IC50 |
55 nM
Compound: 23bb
|
Cytotoxicity against human H460 cells after 72 hrs by MTT assay
Cytotoxicity against human H460 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| Ramos | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human Ramos cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human Ramos cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| Ramos | IC50 |
71 nM
Compound: 23bb
|
Cytotoxicity against human Ramos cells after 72 hrs by MTT assay
Cytotoxicity against human Ramos cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| RPMI-8226 | IC50 |
15 nM
Compound: 23bb
|
Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay
Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| RPMI-8226 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| SK-BR-3 | IC50 |
22 nM
Compound: 23bb
|
Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay
Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| SK-OV-3 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
| SK-OV-3 | IC50 |
50 nM
Compound: 23bb
|
Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| U-266 | IC50 |
14 nM
Compound: 23bb
|
Cytotoxicity against human U266 cells after 72 hrs by MTT assay
Cytotoxicity against human U266 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| U-266 | IC50 |
31 nM
Compound: 27; SKLB-23bb
|
Antiproliferative activity against human U-266 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human U-266 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34101463] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1815580-06-3
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Appearance Solid
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Molecular Weight 396.44
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Formula C21H24N4O4
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Color Light yellow to yellow
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SMILES
CN(C1=CC(OCCCC(NO)=O)=C(OC)C=C1)C2=NC(C)=NC3=CC=CC=C32
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 32 mg/mL (80.72 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 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 |