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| Targets |
SB-429201 primarily targets histone deacetylase 1 (HDAC1). HDAC1 is a class I histone deacetylase that plays a crucial role in the regulation of gene expression by removing acetyl groups from histone proteins. By inhibiting HDAC1, SB-429201 can alter chromatin structure and gene transcription. Some sources list its target as FGFR1 (Fibroblast Growth Factor Receptor 1). It exhibits at least a 20-fold selectivity for HDAC1 over HDAC3 and HDAC8.
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| ln Vitro |
SB-429201 is a potent inhibitor of HDAC1 with an IC50 of approximately 1.5 μM. It displays at least a 20-fold selectivity for HDAC1 over other class I isoforms, including HDAC3 and HDAC8. This selectivity makes it a valuable tool for dissecting the specific roles of HDAC1 in various biological processes. Some sources indicate it is a selective inhibitor of FGFR1.
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| ln Vivo |
Specific in vivo data for SB-429201 is not detailed in the provided search results. However, as an HDAC1 inhibitor, it has potential applications in cancer research, and its in vivo efficacy would be evaluated in relevant animal models. Its potential use in oncology is mentioned, particularly for cancers driven by aberrant FGFR1 signaling, suggesting it may have been tested in vivo for such indications.
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| Enzyme Assay |
The in vitro activity of SB-429201 is assessed using enzyme inhibition assays with purified HDAC1. The compound is incubated with the enzyme and a substrate, and the extent of inhibition is measured. The IC50 value of approximately 1.5 μM for HDAC1 is determined from these assays. Selectivity is confirmed by testing the compound against other HDAC isoforms, such as HDAC3 and HDAC8.
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| Cell Assay |
While the primary characterization of SB-429201 is through biochemical enzyme assays, its activity can also be studied in cell-based systems. In cellular assays, the compound's ability to inhibit HDAC1 can be measured by assessing the acetylation status of histone proteins or specific non-histone substrates. Cell proliferation and viability assays can be used to evaluate its antipotential in cancer cell lines.
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| Animal Protocol |
Specific in vivo animal experiment protocols for SB-429201 are not provided in the search results. However, typical studies would involve administering the compound to tumor-bearing mice in xenograft models. Tumor growth inhibition would be monitored, and pharmacodynamic markers such as histone acetylation in tumor tissues could be measured to confirm target engagement.
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| ADME/Pharmacokinetics |
SB-429201 has a molecular weight of 436.50 and a molecular formula of C28H24N2O3. It has a purity of >98%. The powder should be stored at -20°C for up to 3 years, and in solution at -20°C for up to 6 months. It is soluble in DMSO. The IUPAC name is N-(4-phenoxyphenyl)-4-(3-phenylpropanoylamino)benzamide.
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| Toxicity/Toxicokinetics |
SB-429201 is a potent and selective HDAC1 inhibitor, but its toxicity profile is not detailed in the provided sources. As with other HDAC inhibitors, potential toxicities could include effects on normal cell cycle regulation and gene expression. Its selectivity for HDAC1 may offer a better safety profile compared to pan-HDAC inhibitors. However, comprehensive toxicological studies would be required for its development as a therapeutic agent.
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| References |
: J Pharmacol Exp Ther. 2003 Nov;307(2):720-8.
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| Additional Infomation |
SB-429201 (CAS#: 1027971-34-1) is a potent and selective inhibitor of histone deacetylase 1 (HDAC1) with an IC50 of approximately 1.5 μM. It displays at least a 20-fold selectivity for HDAC1 over other class I isoforms like HDAC3 and HDAC8. It is a valuable research tool for studying HDAC1-specific functions. Some sources also describe it as a selective FGFR1 inhibitor, indicating potential ambiguity in its reported target.
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| Molecular Formula |
C28H24N2O3
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| Molecular Weight |
436.501767158508
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| Exact Mass |
436.178
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| CAS # |
1027971-34-1
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| PubChem CID |
10388312
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
596
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CCC1C=CC=CC=1)NC1C=CC(C(NC2C=CC(=CC=2)OC2C=CC=CC=2)=O)=CC=1
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| InChi Key |
YPXLCXVERGDWHW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H24N2O3/c31-27(20-11-21-7-3-1-4-8-21)29-23-14-12-22(13-15-23)28(32)30-24-16-18-26(19-17-24)33-25-9-5-2-6-10-25/h1-10,12-19H,11,20H2,(H,29,31)(H,30,32)
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| Chemical Name |
N-(4-phenoxyphenyl)-4-(3-phenylpropanoylamino)benzamide
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| Synonyms |
SB429201 SB 429201 SB-429201
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~229.10 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2910 mL | 11.4548 mL | 22.9095 mL | |
| 5 mM | 0.4582 mL | 2.2910 mL | 4.5819 mL | |
| 10 mM | 0.2291 mL | 1.1455 mL | 2.2910 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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