I-BET-762BET inhibitor,highly potent CAS# 1260907-17-2 |
- RVX-208
Catalog No.:BCC4475
CAS No.:1044870-39-4
- Bromodomain Inhibitor, (+)-JQ1
Catalog No.:BCC1132
CAS No.:1268524-70-4
- I-BET151 (GSK1210151A)
Catalog No.:BCC4476
CAS No.:1300031-49-5
- GSK1324726A
Catalog No.:BCC4038
CAS No.:1300031-52-0
- PFI-1 (PF-6405761)
Catalog No.:BCC2225
CAS No.:1403764-72-6
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1260907-17-2 | SDF | Download SDF |
PubChem ID | 46943432 | Appearance | Powder |
Formula | C22H22ClN5O2 | M.Wt | 423.9 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | I-BET 762; Molibresib | ||
Solubility | DMSO : 33.33 mg/mL (78.63 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
Chemical Name | 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide | ||
SMILES | CCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)C | ||
Standard InChIKey | AAAQFGUYHFJNHI-SFHVURJKSA-N | ||
Standard InChI | InChI=1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | I-BET-762 is a highly potent inhibitor of bromo and extra C-terminal domain (BET) family with IC50 values of 32.5–42.5 nM. | |||||
Targets | BET | |||||
IC50 | 32.5–42.5 nM |
I-BET-762 Dilution Calculator
I-BET-762 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.359 mL | 11.7952 mL | 23.5905 mL | 47.1809 mL | 58.9762 mL |
5 mM | 0.4718 mL | 2.359 mL | 4.7181 mL | 9.4362 mL | 11.7952 mL |
10 mM | 0.2359 mL | 1.1795 mL | 2.359 mL | 4.7181 mL | 5.8976 mL |
50 mM | 0.0472 mL | 0.2359 mL | 0.4718 mL | 0.9436 mL | 1.1795 mL |
100 mM | 0.0236 mL | 0.118 mL | 0.2359 mL | 0.4718 mL | 0.5898 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
I-BET-762 is a highly potent inhibitor of BET with IC50 values of 32.5–42.5 nM [1].
I-BET-762 is found to have high affinity with BET (Kd of 50.5–61.3 nM). It binds to the acetyl-lysine (AcK)-binding pocket of BET and competes with AcK. The structure of I-BET-762 allows it to bind with BET in ratio of 2:1 results in the high affinity of it. I-BET-762 also has high selectivity, it has no interaction with other bromodomain-containing proteins. I-BET-762 is reported to downregulate the expression of the genes which are induced by LPS, thus causing the decreased expression of LPS-inducible cytokines and chemokines. In vivo assay shows that I-BET-762 has the anti-inflammatory potential. Treatment of I-BET-762 can cure the mice which have started to develop symptoms of inflammatory disease [1].
References:
[1] Nicodeme E, Jeffrey KL, Schaefer U, Beinke S, Dewell S, Chung CW, Chandwani R, Marazzi I, Wilson P, Coste H, White J, Kirilovsky J, Rice CM, Lora JM, Prinjha RK, Lee K, Tarakhovsky A. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468 (7327):1119-23.
- 6-O-Methylcerevisterol
Catalog No.:BCN6139
CAS No.:126060-09-1
- Atractyloside A
Catalog No.:BCN5383
CAS No.:126054-77-1
- GSK 525768A
Catalog No.:BCC1603
CAS No.:1260530-25-3
- 3-O-beta-Allopyranosyl-(1->4)-beta-oleandropyranosyl-11-O-isobutyryl-12-O-acetyltenacigenin B
Catalog No.:BCN6765
CAS No.:1260252-18-3
- Birinapant (TL32711)
Catalog No.:BCC2250
CAS No.:1260251-31-7
- TCS 21311
Catalog No.:BCC2443
CAS No.:1260181-14-3
- 3-Oxo-21alpha-methoxy-24,25,26,27-tetranortirucall-7-ene-23(21)-lactone
Catalog No.:BCN7028
CAS No.:1260173-73-6
- TAK-438
Catalog No.:BCC1182
CAS No.:1260141-27-2
- 28-Deoxonimbolide
Catalog No.:BCN4717
CAS No.:126005-94-5
- Carminic acid
Catalog No.:BCN6541
CAS No.:1260-17-9
- Phlegmanol C
Catalog No.:BCN6138
CAS No.:1260-05-5
- Polygalic acid
Catalog No.:BCN3172
CAS No.:1260-04-4
- Rubiyunnanin C
Catalog No.:BCN8045
CAS No.:1261030-04-9
- 11-Oxo-mogroside V
Catalog No.:BCN2509
CAS No.:126105-11-1
- Siamenoside I
Catalog No.:BCN2540
CAS No.:126105-12-2
- GNF179
Catalog No.:BCC5175
CAS No.:1261114-01-5
- BAPTA-AM
Catalog No.:BCC5456
CAS No.:126150-97-8
- Icariside E5
Catalog No.:BCN6140
CAS No.:126176-79-2
- Spiranthol A
Catalog No.:BCN7893
CAS No.:126192-35-6
- LY2886721
Catalog No.:BCC3807
CAS No.:1262036-50-9
- Ginsenoside Rg4
Catalog No.:BCN2713
CAS No.:126223-28-7
- Agrimonolide 6-O-glucoside
Catalog No.:BCN6141
CAS No.:126223-29-8
- INCB3344
Catalog No.:BCC1648
CAS No.:1262238-11-8
- Uralsaponin C
Catalog No.:BCN7906
CAS No.:1262326-46-4
Bromodomain inhibitors, JQ1 and I-BET 762, as potential therapies for pancreatic cancer.[Pubmed:28254412]
Cancer Lett. 2017 May 28;394:76-87.
Bromodomain inhibitors (JQ1 and I-BET 762) are a new generation of selective, small molecule inhibitors that target BET (bromodomain and extra terminal) proteins. By impairing their ability to bind to acetylated lysines on histones, bromodomain inhibitors interfere with transcriptional initiation and elongation. BET proteins regulate several genes responsible for cell cycle, apoptosis and inflammation. In this study, JQ1 and I-BET 762 decreased c-Myc and p-Erk 1/2 protein levels and inhibited proliferation in pancreatic cancer cells. The tumor microenvironment is known to play an important role in pancreatic cancer, and these drugs suppressed the production of nitric oxide and a variety of inflammatory cytokines, including IL-6, CCL2, and GM-CSF, in both immune and pancreatic cancer cells in vitro. Notably, the bromodomain inhibitors also reduced protein levels of p-Erk 1/2 and p-STAT3 in mouse models of pancreatic cancer. All of these proteins are essential for tumor promotion, progression and metastasis. In conclusion, the bromodomain inhibitors JQ1 and I-BET 762 targeted and suppressed multiple pathways in pancreatic cancer. I-BET 762 and a number of other bromodomain inhibitors are currently being tested in several clinical trials, making them potentially promising drugs for the treatment of pancreatic cancer, an often-fatal disease.