NI-42 |
Catalog No.GC36734
One-Click Copy Product Info
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BRPF에 대한 구조적으로 직교하는 화학 프로브인 NI-42(화합물 13-d)는 BRPF의 BRD에 대한 편향되고 강력한 억제제입니다(BRPF1/2/3의 IC50=7.9/48/260nM; BRPF1의 Kds /2/3=40/210/940 nM) 비클래스 IV BRD 단백질에 비해 탁월한 선택성을 제공합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1884640-99-6
Sample solution is provided at 25 µL, 10mM.
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NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins[1]. BRPF1|7.9 nM (IC50)|BRPF2|48 nM (IC50)|BRPF3|260 nM (IC50)|BRPF1|40 nM (Kd)|BRPF2|210 nM (Kd)|BRPF3|940 nM (Kd)|BRD4 (BD1)|4500 nM (IC50)|BRD7|82 nM (IC50)|BRD9|310 nM (IC50)|BRD9|1130 nM (Kd)
NI-42 shows IC50s of 82, 310, and 4500 nM for BRD7, BRD9, and BRD4 (BD1), respectively, and has a Kd of 1130 nM for BRD9[1].
[1]. Igoe N, et al. Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies. J Med Chem. 2017 Jan 26;60(2):668-680.
| Cas No. | 1884640-99-6 | SDF | |
| Canonical SMILES | O=S(C1=CC=C(C#N)C=C1)(NC2=CC=C(N(C)C(C(C)=C3)=O)C3=C2)=O | ||
| Formula | C18H15N3O3S | M.Wt | 353.4 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8297 mL | 14.1483 mL | 28.2965 mL |
| 5 mM | 565.9 μL | 2.8297 mL | 5.6593 mL |
| 10 mM | 283 μL | 1.4148 mL | 2.8297 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)