iPAF1C
Based on 1 Customer Validation
iPAF1C is a inhibitor of the polymerase-associated factor 1 complex (PAF1C) with specific targeting to the PAF1 binding groove of CTR9 (a key subunit of PAF1C). iPAF1C disrupts PAF1C assembly by interfering with the PAF1-CTR9 interaction. iPAF1C selectively impairs BRD4-mediated recruitment of PAF1 to chromatin at hypoxia-responsive genes and inhibits RNA polymerase II (RNAPII) pause release. iPAF1C increases the population of HIV-1 NL4.3 Nef-IRES-GFP infected primary human CD4+T cells in a dose-dependent manner. PAF1C can be used for the study of infection and diseases associated with abnormal hypoxic adaptation (e.g., cancers, neurological disorders).
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- Purity: 99.59%
- CAS No.: 950403-60-8
- 화학식: C27H26BrFN4O
- 분자량:521.42
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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Highly Selective Inhibitors Library
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Biological Activity
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RNA Polymerase |
iPAF1C (20 μM, 16 h) mimics the effect of PAF1 shRNA transduction, inducing global release of promoter-proximal paused RNA Pol II into gene bodies and increasing the pause-release ratio (PRR) of RNA Pol II in HCT116 cells[1].
iPAF1C (20 μM, 3 h) specifically enhances the thermostability of CTR9 (a subunit of PAF1C)[1].
iPAF1C (20 μM, 16 h) disrupts the interaction between PAF1 and CTR9 in DLD1 cells engineered with an auxin-inducible degron (AID) tag at the endogenous PAF1 locus[1].
iPAF1C (6.25-12.5 μM) increases the population of HIV-1 NL4.3 Nef-IRES-GFP infected primary human CD4+T cells in a dose-dependent manner[1].
iPAF1C (20 μM, 6 h) impairs PAF1 chromatin recruitment to hypoxia-responsive genes in both untreated pIAA7-tagged BRD4 DLD-1 cells and auxin-treated BRD4 C mutant-complemented DLD-1 cells under hypoxic conditions[2].
iPAF1C (20 μM, 6 h) impairs transcriptional elongation by RNAPII at hypoxia-responsive genes in pIAA7-tagged BRD4 DLD-1 cells under hypoxic conditions[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 950403-60-8
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Appearance Solid
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분자량 521.42
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화학식 C27H26BrFN4O
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Color White to off-white
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SMILES
O=C(C1CCN(CC1)C2=NC3=C(N2CC4=CC(F)=CC=C4)C=CC=C3)NC5=CC=C(C(C)=C5)Br
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (95.89 mM; ultrasonic and warming and heat to 60°C; 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 (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Shimaa H A Soliman, et al. Enhancing HIV-1 latency reversal through regulating the elongating RNA Pol II pause-release by a small-molecule disruptor of PAF1C. Sci Adv. 2023 Mar 10;9(10):eadf2468. [Content Brief]
[2]. Soliman SHA, et al. Transcriptional elongation control of hypoxic response. Proc Natl Acad Sci U S A. 2024 Apr 9;121(15):e2321502121. [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 | 1.9178 mL | 9.5892 mL | 19.1784 mL | 47.9460 mL |
| 5 mM | 0.3836 mL | 1.9178 mL | 3.8357 mL | 9.5892 mL | |
| 10 mM | 0.1918 mL | 0.9589 mL | 1.9178 mL | 4.7946 mL | |
| 15 mM | 0.1279 mL | 0.6393 mL | 1.2786 mL | 3.1964 mL | |
| 20 mM | 0.0959 mL | 0.4795 mL | 0.9589 mL | 2.3973 mL | |
| 25 mM | 0.0767 mL | 0.3836 mL | 0.7671 mL | 1.9178 mL | |
| 30 mM | 0.0639 mL | 0.3196 mL | 0.6393 mL | 1.5982 mL | |
| 40 mM | 0.0479 mL | 0.2397 mL | 0.4795 mL | 1.1986 mL | |
| 50 mM | 0.0384 mL | 0.1918 mL | 0.3836 mL | 0.9589 mL | |
| 60 mM | 0.0320 mL | 0.1598 mL | 0.3196 mL | 0.7991 mL | |
| 80 mM | 0.0240 mL | 0.1199 mL | 0.2397 mL | 0.5993 mL |
iPAF1C Related Classifications
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