| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
SENP1[1]
SENP1 (Sentrin/SUMO-specific protease 1). SENP1-IN-1 is a specific inhibitor of SENP1, which is a key enzyme in the SUMOylation cycle. It blocks the isopeptidase activity that cleaves SUMO from substrate proteins. |
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| ln Vitro |
Tumor cells may be more sensitive to radiation when SENP1-IN-1 is present[1]. Hella cells are cytotoxic to SENP1-IN-1 (0.7–20 μM; 72 hours) with an IC50 of greater than 20 μM[1].
SENP1-IN-1 (compound 29, extracted from patent CN110627860) is a specific inhibitor of the deSUMOylation protease SENP1. By inhibiting SENP1, it prevents the removal of SUMO groups from target proteins, leading to an accumulation of SUMOylated proteins in cells. This alteration in the SUMOylation landscape can modulate the DNA damage response, apoptosis, and other signaling pathways. The IC50 value for SENP1 inhibition is not detailed in the supplier literature. |
| ln Vivo |
In vivo, SENP1-IN-1 has been developed for the purpose of enhancing tumor radiosensitivity. By inhibiting SENP1 and altering SUMOylation, it may make cancer cells more susceptible to the effects of ionizing radiation, thereby improving the efficacy of radiotherapy. Specific in vivo efficacy data (e.g., tumor growth delay in xenograft models) are not detailed in the supplier literature. Further characterization is needed.
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| Enzyme Assay |
SENP1-IN-1 is evaluated using cell-free fluorometric assays. Recombinant SENP1 is incubated with a fluorogenic substrate that consists of a SUMO peptide linked to a fluorophore such as AMC. SENP1-IN-1 is added at varying concentrations (0.1-100 uM). The reaction is monitored continuously at 380 nm excitation and 460 nm emission. An increase in fluorescence indicates deSUMOylation, which is inhibited by the compound. The IC50 for SENP1 inhibition is calculated from the dose-response curve.
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| Cell Assay |
Cell Cytotoxicity Assay [1]
Cell Types: Hela cells Tested Concentrations: 0.7 μM, 2.2 μM, 6.6 μM, 20 μM Incubation Duration: 72 hrs (hours) Experimental Results: IC50>20 μM For cellular assays, cancer cells (e.g., HeLa, A549) are treated with SENP1-IN-1 (1-100 uM) for 24-48 hours. The global levels of SUMO1, SUMO2/3, and SUMOylated proteins are assessed by Western blot. An increase in conjugated SUMO is expected. To test the radiosensitizing effect, cells are irradiated with increasing doses (0-10 Gy) in the presence or absence of SENP1-IN-1. Clonogenic survival assays are performed. A reduction in the surviving fraction at a given radiation dose indicates radiosensitization. |
| Animal Protocol |
For in vivo efficacy studies, SENP1-IN-1 can be formulated in a vehicle such as 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline. It would be administered intraperitoneally to mice bearing subcutaneous tumor xenografts (e.g., A549 lung cancer). Local tumor irradiation is performed with a single dose or fractionated doses. Tumor growth is monitored over time. An increase in tumor growth delay in the combination treatment group (inhibitor + radiation) compared to radiation alone indicates radiosensitization. Tumors are harvested for analysis of SUMOylation levels.
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| ADME/Pharmacokinetics |
SENP1-IN-1 has a molecular formula of C35H58N2O4 and a molecular weight of 570.85 g/mol. It is soluble in DMSO (90 mg/mL). The compound is stored as a powder at -20degC (stable for 3 years) or in solution at -80degC (6 months). Detailed pharmacokinetic parameters (half-life, oral bioavailability) are not reported in the supplier literature. It is supplied as a solid.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for SENP1-IN-1 are not available. It is intended for research use only and not for human consumption. Standard safety precautions for handling research chemicals should be followed, including the use of gloves and eye protection. The compound may be irritating to the eyes, skin, and respiratory tract. As a SENP1 inhibitor, it could potentially cause off-target effects on normal tissues.
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| References | |
| Additional Infomation |
SENP1-IN-1 is a research-grade chemical, not an FDA-approved drug. It is extracted from patent CN110627860, where it is described as compound 29. The compound is part of a series of inhibitors developed for enhancing tumor radiosensitivity. SENP1 is an attractive target because it regulates the DNA damage response and is often upregulated in cancer cells, contributing to their resistance to radiation and chemotherapy.
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| Molecular Formula |
C35H58N2O4
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| Molecular Weight |
570.846030712128
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| Exact Mass |
570.439
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| CAS # |
2416910-69-3
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| PubChem CID |
162642615
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| Appearance |
White to off-white solid powder
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| LogP |
5.9
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
41
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| Complexity |
1090
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C([C@]12CC[C@@H](C)[C@H](C)[C@@]1([H])C1=CC[C@]3([H])[C@]4(CC[C@H](O)C(C)(C)[C@]4([H])CC[C@@]3(C)[C@]1(C)CC2)C)(=O)NCC(=O)N(C)CCO
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| InChi Key |
GYEWLVQWUVDKKH-SKHUFZRLSA-N
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| InChi Code |
InChI=1S/C35H58N2O4/c1-22-11-16-35(30(41)36-21-28(40)37(8)19-20-38)18-17-33(6)24(29(35)23(22)2)9-10-26-32(5)14-13-27(39)31(3,4)25(32)12-15-34(26,33)7/h9,22-23,25-27,29,38-39H,10-21H2,1-8H3,(H,36,41)/t22-,23+,25+,26-,27+,29+,32+,33-,34-,35+/m1/s1
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| Chemical Name |
(1S,2R,4aS,6aR,6aS,6bR,8aR,10S,12aR,14bS)-10-hydroxy-N-[2-[2-hydroxyethyl(methyl)amino]-2-oxoethyl]-1,2,6a,6b,9,9,12a-heptamethyl-2,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydro-1H-picene-4a-carboxamide
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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 (175.18 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 | 1.7518 mL | 8.7589 mL | 17.5177 mL | |
| 5 mM | 0.3504 mL | 1.7518 mL | 3.5035 mL | |
| 10 mM | 0.1752 mL | 0.8759 mL | 1.7518 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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