KMR-206
Based on 1 Customer Validation
KMR-206 is a PARP7 inhibitor with an IC50 of 13.7 nM. KMR-206 relieves AHR-mediated transcriptional repression and enhances CYP1A1 expression in the presence of TCDD. KMR-206 induces the STING-dependent IFN-β signaling pathway and increases the levels of STAT1, pSTAT1 and nuclear PARP7 in cancer cells. KMR-206 reduces the viability of lung adenocarcinoma cells, enhances radiation-induced immunogenic signals, and induces the production of immunogenic signals in glioblastoma cancer stem cells. KMR-206 destabilizes FRA1 to increase IRF1 levels and promotes the IRF3-CBP/p300 interaction. KMR-206 can be used in studies related to lung adenocarcinoma and glioblastoma.
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- Purity: 98.86%
- CAS No.: 2992741-10-1
- 화학식: C29H23FN6O2
- 분자량:506.53
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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PARP7 13.7 nM (IC50) |
STAT1 |
IFNAR1 |
KMR-206 potently and selectively inhibits the catalytic activity of purified PARP7 in vitro, with an IC50 of 13.7 nM[1].
KMR-206 (0.001-0.3 μM; duration sufficient to measure MARylation) inhibits the auto-MARylation of GFP-PARP7 in HEK 293T cells with an EC50 of 8 nM, and upregulates GFP-PARP7 protein levels in a dose-dependent manner[1].
KMR-206 (0.1-1000 nM; 24 h) reverses AHR ligand-mediated transcriptional inhibition of CYP1A1 in WT MEFs in a dose-dependent manner in vitro, with a saturating effect observed at 100 nM[1].
KMR-206 (100 nM; 24 h) increases the IFN-β mRNA level in WT MEFs[1].
KMR-206 (0.01-0.3 μM; 16 h) dose-dependently induces the IFN-β signaling pathway in CT-26 cells, including upregulating STAT1/pSTAT1 levels, STING-dependent IFN-β secretion, and ISRE reporter gene activity[1].
KMR-206 (0.01-0.3 μM; 16 h) upregulates the endogenous PARP7 protein level in CT-26 cells in a dose-dependent manner[1].
KMR-206 (6 days) reduces the viability of NCI-H1373 cells in a dose-dependent manner with an EC50 of 104 nM, but exerts no effect on the viability of CT-26 cells[1].
KMR-206 (300 nM; imaged at 0, 30, 120 min post-treatment) alters the nuclear localization of GFP-PARP7 in HeLa cells, converting punctate nuclear localization into a diffuse pan-nuclear pattern within 30 min post-treatment[1].
KMR-206 (300 nM; added 2 h prior to irradiation and removed 24 h after irradiation) sensitizes human glioblastoma cell lines U251, T98G and KALS-1 to X-ray irradiation[2].
KMR-206 (administered 2 h before the first radiation fraction and maintained for 72 h after the last fraction) enhances radiotherapy-induced IFN-I and pro-inflammatory gene expression in U251, T98G and KALS-1 human glioblastoma cell lines, and exerts cell line-specific effects on gene targets and pathway enrichment[2].
KMR-206 (300 nM; added 2 h prior to irradiation and maintained for 72 h after irradiation) enhances radiation-induced activation of the IFN-I pathway in T98G cells and also enhances IFN-I pathway activation in KALS-1 cells[2].
Supernatants generated from the combined treatment of human glioblastoma cell lines U251, T98G and KALS-1 with KMR-206 (300 nM; added 2 h prior to the first radiation fraction and maintained for 72 h after the last fraction) and 3 × 8 Gy X-rays activate primary human NK, NKT and monocyte populations, with cell line-specific activation characteristics[2].
Combination of KMR-206 (administered 2 h before the first radiotherapy fraction and maintained for 72 h after the last fraction) with X-ray irradiation induces activation of the IFN-I pathway and expression of proinflammatory cytokines in STING-low-expressing LK17 patient-derived human glioblastoma cancer stem cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK 293T cells expressing GFP-PARP7
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Concentration:0.001, 0.01, 0.03, 0.1, 0.3 μM
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Incubation Time:duration sufficient to measure MARylation
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Result:Induced a dose-dependent decrease in GFP-PARP7 auto-MARylation with an EC50 of 8 nM.
Caused a dose-dependent increase in GFP-PARP7 protein levels.
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Cell Line:WT mouse embryonic fibroblasts (MEFs)
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Concentration:100 nM
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Incubation Time:24 h (alone); 4 h (with 100 ng/mL 3pRNA or 5 μg/mL cGAMP)
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Result:Induced a 3-fold increase in IFN-β mRNA when used alone.
Caused a synergistic induction of IFN-β mRNA when co-treated with 3pRNA or cGAMP, with drastically higher levels than either treatment alone.
Chemical Information
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CAS No. 2992741-10-1
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Appearance Solid
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분자량 506.53
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화학식 C29H23FN6O2
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Color White to off-white
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SMILES
N#CC1=CC=C(N2CCN(C(C3=CC(CC4=NNC(C5=C4C=C(C#CC)C=C5)=O)=CC=C3F)=O)CC2)N=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (98.71 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
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.
순도&문서
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Sanderson DJ, et al. Structurally distinct PARP7 inhibitors provide new insights into the function of PARP7 in regulating nucleic acid-sensing and IFN-β signaling. Cell Chem Biol. 2023;30(1):43-54.e8. [Content Brief]
[2]. Lippert L, et al. PARP7 inhibition and a STING agonist potentiate radiation-induced immunogenicity in glioblastoma. Oncoimmunology. 2026;15(1):2656053. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9742 mL | 9.8711 mL | 19.7422 mL | 49.3554 mL |
| 5 mM | 0.3948 mL | 1.9742 mL | 3.9484 mL | 9.8711 mL | |
| 10 mM | 0.1974 mL | 0.9871 mL | 1.9742 mL | 4.9355 mL | |
| 15 mM | 0.1316 mL | 0.6581 mL | 1.3161 mL | 3.2904 mL | |
| 20 mM | 0.0987 mL | 0.4936 mL | 0.9871 mL | 2.4678 mL | |
| 25 mM | 0.0790 mL | 0.3948 mL | 0.7897 mL | 1.9742 mL | |
| 30 mM | 0.0658 mL | 0.3290 mL | 0.6581 mL | 1.6452 mL | |
| 40 mM | 0.0494 mL | 0.2468 mL | 0.4936 mL | 1.2339 mL | |
| 50 mM | 0.0395 mL | 0.1974 mL | 0.3948 mL | 0.9871 mL | |
| 60 mM | 0.0329 mL | 0.1645 mL | 0.3290 mL | 0.8226 mL | |
| 80 mM | 0.0247 mL | 0.1234 mL | 0.2468 mL | 0.6169 mL |
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