| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
REV7/REV3L-IN-1 targets the REV7-REV3L protein-protein interaction, a critical component of the translesion DNA synthesis (TLS) pathway. REV7 (also known as MAD2L2) and REV3L form the catalytic core of DNA polymerase zeta (Pol zeta), which is responsible for TLS, a DNA damage tolerance mechanism that allows cells to replicate past DNA lesions. By inhibiting the REV7-REV3L interaction, REV7/REV3L-IN-1 blocks Pol zeta activity, thereby preventing TLS and promoting sensitivity to DNA-damaging agents. This mechanism makes the compound a valuable tool for studying DNA repair and overcoming chemoresistance.
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| ln Vitro |
In vitro, REV7/REV3L-IN-1 inhibits the REV7-REV3L protein-protein interaction, blocking translesion DNA synthesis (TLS) activity. The compound sensitizes cancer cells to DNA-damaging agents such as cisplatin and other chemotherapeutic drugs. By inhibiting TLS, REV7/REV3L-IN-1 prevents the replication of damaged DNA, leading to increased DNA damage and cell death in cancer cells. These in vitro properties establish REV7/REV3L-IN-1 as a valuable tool for studying TLS and for potential therapeutic applications in overcoming chemoresistance.
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| ln Vivo |
In vivo, REV7/REV3L-IN-1 has been studied for its potential to sensitize tumors to DNA-damaging agents. By inhibiting the REV7-REV3L interaction, the compound blocks translesion DNA synthesis, thereby promoting sensitivity to chemotherapeutic drugs. Detailed in vivo efficacy data are limited in publicly available literature. REV7/REV3L-IN-1 is for research purposes only and is not approved for clinical use.
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| Enzyme Assay |
REV7/REV3L-IN-1 is not typically used in standard receptor binding assays. Its activity is assessed through protein-protein interaction assays or cell-based assays measuring TLS activity. In protein-protein interaction assays, the compound's ability to disrupt the REV7-REV3L interaction is measured using methods such as fluorescence polarization, AlphaScreen, or surface plasmon resonance (SPR). The compound is incubated with REV7 and REV3L proteins at varying concentrations, and the extent of interaction is measured. IC50 values are calculated from concentration-response curves.
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| Cell Assay |
Cellular assays for REV7/REV3L-IN-1 are performed using cancer cell lines that are sensitive to DNA-damaging agents. Cells are cultured in appropriate media and treated with REV7/REV3L-IN-1 at varying concentrations, alone or in combination with DNA-damaging agents such as cisplatin. Cell viability and proliferation are assessed using standard assays such as MTT, CellTiter-Glo, or colony formation assays. DNA damage and repair are assessed by measuring gamma-H2AX foci formation or by comet assays. TLS activity may be assessed using reporter assays.
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| Animal Protocol |
In vivo studies with REV7/REV3L-IN-1 are conducted in mouse xenograft models using cancer cell lines. REV7/REV3L-IN-1 is administered via appropriate routes (e.g., intraperitoneal or oral) at defined doses and schedules, alone or in combination with DNA-damaging agents. Tumor growth is monitored by caliper measurements, and tumor volumes are calculated. Tumor tissues are collected for assessment of DNA damage and repair markers by immunohistochemistry or Western blot. Pharmacokinetic parameters are determined from plasma samples collected at various time points.
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| ADME/Pharmacokinetics |
REV7/REV3L-IN-1 has a molecular weight of 406.48 and a molecular formula of C22H23FN4O3. The compound is an inhibitor of the REV7-REV3L protein-protein interaction. Detailed pharmacokinetic data for REV7/REV3L-IN-1 are not extensively documented in publicly available literature. The compound is soluble in DMSO. It should be stored at -20degC. REV7/REV3L-IN-1 is intended for research use only.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for REV7/REV3L-IN-1 are not extensively documented in publicly available sources. The compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and adherence to institutional biosafety and chemical hygiene guidelines. The compound has a purity of ≥98%.
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| References | |
| Additional Infomation |
REV7/REV3L-IN-1 is a small-molecule inhibitor targeting the REV7-REV3L protein-protein interaction, which is involved in the translesion DNA synthesis (TLS) pathway. By inhibiting the REV7-REV3L interaction, the compound blocks DNA damage tolerance and promotes sensitivity to DNA-damaging agents. REV7/REV3L-IN-1 is used as a research tool to study the role of TLS in DNA repair and cancer therapy, with potential applications in overcoming chemoresistance. The compound is for research purposes only.
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| Molecular Formula |
C19H21N3O3S
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|---|---|
| Molecular Weight |
371.453343153
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| Exact Mass |
371.13
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| CAS # |
1979192-13-6
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| PubChem CID |
134141027
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
591
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C=C(C2=CC=C(C)O2)C2=C1N=CN(C2=O)CC1CCN(C(C)=O)CC1
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| InChi Key |
FCAGATFCNDPZOG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H21N3O3S/c1-12-3-4-16(25-12)15-10-26-18-17(15)19(24)22(11-20-18)9-14-5-7-21(8-6-14)13(2)23/h3-4,10-11,14H,5-9H2,1-2H3
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| Chemical Name |
3-[(1-acetylpiperidin-4-yl)methyl]-5-(5-methylfuran-2-yl)thieno[2,3-d]pyrimidin-4-one
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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 : ~7.14 mg/mL (~19.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6922 mL | 13.4608 mL | 26.9215 mL | |
| 5 mM | 0.5384 mL | 2.6922 mL | 5.3843 mL | |
| 10 mM | 0.2692 mL | 1.3461 mL | 2.6922 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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