PeptideDB

SAHA-OH 2857098-30-5

SAHA-OH 2857098-30-5

CAS No.: 2857098-30-5

SAHA-OH is a selective HDAC6 inhibitor (IC50=23 nM) with 10-47 times selectivity for HDAC6 compared to HDAC1, 2, 3 and 8
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SAHA-OH is a selective HDAC6 inhibitor (IC50=23 nM) with 10-47 times selectivity for HDAC6 compared to HDAC1, 2, 3 and 8. SAHA-OH exhibits anti-inflammatory effect and reduces macrophage apoptosis.

Physicochemical Properties


Molecular Formula C15H22N2O4
Molecular Weight 294.35
CAS # 2857098-30-5
Appearance Typically exists as solid at room temperature
HS Tariff Code 2934.99.9001
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)

Biological Activity


Targets HDAC6 23 nM (IC50) HDAC1 237 nM (IC50) HDAC3 359 nM (IC50) HDAC2 399 nM (IC50) HDAC8 1070 nM (IC50)
ln Vitro In bone marrow macrophages, SAHA-OH (0.67-10.76 μM; 51 h) exhibits inhibition[1]. When administered at a concentration of 0.01 μM for three hours, bone marrow macrophages (BMMØs) secrete less IL-6, TNFα, IFNβ, IL-1β, IL-10, MCP-1 (CCL2), and GROα (CXCL1)[1]. Treatment with SAHA-OH (10 μM; 4 or 9 h) causes acetylation of nuclear histone H3 and cytoplasmic α-tubulin[1]. Treatment with SAHA-OH (0-30 μM; 3 h) reduces macrophage apoptosis. B cell death is attenuated by SAHA-OH (0-30 μM; 3 h) treatment[1].
ln Vivo In an LPS-induced endotoxemia animal model, SAHA-OH (intraperitoneal injection; 50 mg/kg; once) therapy lowers plasma proinflammatory cytokine levels and avoids damage to the splenic organs[1].
Cell Assay Cell Viability Assay[1]
Cell Types: BMMØs (bone marrow macrophages)
Tested Concentrations: 0.67-10.76 μM
Incubation Duration: 51 h
Experimental Results: demonstrated IC50 value in unstimulated BMMØs of 1.26 μM, and demonstrated IC50 value in LPS-stimulated BMMØs of 10.76 μM.

Apoptosis Analysis[1]
Cell Types: BMMØs (bone marrow macrophages)
Tested Concentrations: 0-30 μM
Incubation Duration: 3 h
Experimental Results: Resulted in a 24- to 26 -fold increase in cellular viability as compared to the SAHA treatment.

Cell Cytotoxicity Assay[1]
Cell Types: B cells
Tested Concentrations: 0-30 μM
Incubation Duration: 3 h
Experimental Results: Resulted in a 5-fold enhancement in viability and a 3- fold decrease in cell death for the B cell population.

Western Blot Analysis[1]
Cell Types: BMMØs (bone marrow macrophages)
Tested Concentrations: 10 μM
Incubation Duration: 4 or 9 h
Experimental Results: Resulted in the acetylation of α-tubulin. Induced the acetylation of histone H3 compared to no treatment (NT).
Animal Protocol Animal/Disease Models: LPS-induced endotoxemia mouse model[1]
Doses: 50 mg/kg
Route of Administration: intraperitoneal (ip)injection; 50 mg/kg; once
Experimental Results: diminished proinflammatory cytokine secretions by about 50% compared to no treatment (NT) control mice. demonstrated similar architecture as no treatment (NT) control and displayed well-organized lymphoid follicles.
References [1]. Nhu Truong, et al. Modified Suberoylanilide Hydroxamic Acid Reduced Drug-Associated Immune Cell Death and Organ Damage under Lipopolysaccharide Inflammatory Challenge. ACS Pharmacol. Transl. Sci. 2022.

Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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).
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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3973 mL 16.9866 mL 33.9732 mL
5 mM 0.6795 mL 3.3973 mL 6.7946 mL
10 mM 0.3397 mL 1.6987 mL 3.3973 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.