C 21Protein arginine methyltransferase 1 (PRMT1) inhibitor CAS# 1229236-78-5 |
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| Cas No. | 1229236-78-5 | SDF | Download SDF |
| PubChem ID | 90489011 | Appearance | Powder |
| Formula | C90H161ClN36O24 | M.Wt | 2166.94 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 2 mg/ml in water | ||
| Sequence | SGXGKGGKGLGKGGAKRHRKV (Modifica | ||
| SMILES | CC(C)CC(C(=O)NCC(=O)NC(CCCCN)C(=O)NCC(=O)NCC(=O)NC(C)C(=O)NC(CCCCN)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC1=CNC=N1)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(C(C)C)C(=O)O)NC(=O)CNC(=O)C(CCCCN)NC(=O)CNC(=O)CNC(=O)C(CCCCN)NC(=O)CNC(=O)C(CCCNC(=N)CCl)NC(=O)CNC(=O)C(CO)NC(=O)C | ||
| Standard InChIKey | OANJWIVLLOAGEG-CQSMXCMYSA-N | ||
| Standard InChI | InChI=1S/C90H161ClN36O24/c1-50(2)36-63(121-74(137)47-111-79(141)57(22-9-14-30-94)117-70(133)43-107-68(131)41-109-77(139)55(20-7-12-28-92)118-71(134)44-110-80(142)58(25-17-33-103-66(97)38-91)120-73(136)46-113-82(144)65(48-128)116-53(6)129)81(143)112-45-72(135)119-56(21-8-13-29-93)78(140)108-40-67(130)106-42-69(132)115-52(5)76(138)122-59(23-10-15-31-95)83(145)124-62(27-19-35-105-90(100)101)85(147)126-64(37-54-39-102-49-114-54)87(149)125-61(26-18-34-104-89(98)99)84(146)123-60(24-11-16-32-96)86(148)127-75(51(3)4)88(150)151/h39,49-52,55-65,75,128H,7-38,40-48,92-96H2,1-6H3,(H2,97,103)(H,102,114)(H,106,130)(H,107,131)(H,108,140)(H,109,139)(H,110,142)(H,111,141)(H,112,143)(H,113,144)(H,115,132)(H,116,129)(H,117,133)(H,118,134)(H,119,135)(H,120,136)(H,121,137)(H,122,138)(H,123,146)(H,124,145)(H,125,149)(H,126,147)(H,127,148)(H,150,151)(H4,98,99,104)(H4,100,101,105)/t52-,55-,56-,57-,58-,59-,60-,61-,62-,63-,64-,65-,75-/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. |
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| 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. |
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| 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 | Selective protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 1.8 μM). Exhibits five-fold selectivity for PRMT1 over PRMT6 and >250-fold selectivity over PRMT3 and CARM1. |
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Interleukin-6-174G/C Polymorphism Contributes to Periodontitis Susceptibility: An Updated Meta-Analysis of 21 Case-Control Studies.[Pubmed:28050060]
Dis Markers. 2016;2016:9612421.
Introduction. Chronic Periodontitis (CP) is suggested to be related to gene variations. Present study aims to quantitatively estimate the association between interleukin-6- (IL-6-) 174G/C polymorphism and CP susceptibility. Materials and Methods. Pubmed, Embase, and Web of Science were searched up to May 2016. The meta-analyses were performed using STATA 12.0. Results. 21 studies were yielded. Significant associations were found under heterozygote comparison and dominant model in studies fulfilling HWE (GC versus GG: OR = 0.690, 95% CI = 0.560-0.849, P = 0.000; CC + GC versus GG: OR = 0.690, 95% CI = 0.568-0.838, P < 0.001); significant associations were found under heterozygote comparison and dominant model in Caucasian studies fulfilling HWE (GC versus GG: OR = 0.752, 95% CI = 0.577-0.980, P = 0.035; CC + GC versus GG: OR = 0.737, 95% CI = 0.576-0.944, P = 0.016); significant associations were found under allele comparison, heterozygote comparison, and dominant model in Brazilian population (C versus G: OR = 0.648, 95% CI = 0.497-0.845, P = 0.001; GC versus GG: OR = 0.621, 95% CI = 0.441-0.876, P = 0.007; CC + GC versus GG: OR = 0.649, 95% CI = 0.470-0.896, P = 0.009). Conclusion. IL-6 174 polymorphism is associated with CP susceptibility. In Brazilian and Caucasian population, IL-6 174 GG genotype plays as a risk factor to CP.
Six new C-21 steroidal glycosides from Dregea sinensis Hemsl.[Pubmed:28276767]
J Asian Nat Prod Res. 2017 Aug;19(8):745-753.
Six new C-21 steroidal glycosides (1-6) were separated from the root of Dregea sinensis Hemsl. and their structures were elucidated using extensive nuclear magnetic resonance, mass spectrometry, and infrared spectral analyses. Isolated compounds were evaluated for antitumor activity, which showed that compound 3 had moderate activity in Jurkat cells (IC50 19.54 +/- 0.91 muM), and compounds 1-4 had significant effects against IL-2R and TNFR2 (IC50 1.518 +/- 0.06 muM to 5.9 +/- 0.07 muM).
miR-21 increases c-kit(+) cardiac stem cell proliferation in vitro through PTEN/PI3K/Akt signaling.[Pubmed:28168101]
PeerJ. 2017 Jan 5;5:e2859.
The low survival rate of cardiac stem cells (CSCs) in the ischemic myocardium is one of the obstacles in ischemic cardiomyopathy cell therapy. The MicroRNA (miR)-21 and one of its target protein, the tensin homolog deleted on chromosome ten (PTEN), contributes to the proliferation of many kinds of tissues and cell types. It is reported that miR-21 promotes proliferation through PTEN/PI3K/Akt pathway, but its effects on c-kit(+) CSC remain unclear. The authors hypothesized that miR-21 promotes the proliferation in c-kit (+) CSC, and evaluated the involvement of PTEN/PI3K/Akt pathway in vitro. miR-21 up-regulation with miR-21 efficiently mimics accelerated cell viability and proliferation in c-kit (+) CSC, which was evidenced by the CCK-8, EdU and cell cycle analyses. In addition, the over-expression of miR-21 in c-kit (+) CSCs notably down-regulated the protein expression of PTEN although the mRNA level of PTEN showed little change. Gain-of-function of miR-21 also increased the phosphor-Akt (p-Akt) level. Phen, the selective inhibitor of PTEN, reproduced the pro-proliferation effects of miR-21, while PI3K inhibitor, LY294002, totally attenuated the pro-survival effect of miR-21. These results indicate that miR-21 is efficient in promoting proliferation in c-kit(+) CSCs, which is contributed by the PTEN/PI3K/Akt pathway. miR-21 holds the potential to facilitate CSC therapy in ischemic myocardium.
Real-world effectiveness and predictors of sustained virological response with all-oral therapy in 21,242 hepatitis C genotype-1 patients.[Pubmed:27934775]
Antivir Ther. 2017;22(6):481-493.
BACKGROUND: Predictors of sustained virological response (SVR) to all-oral HCV regimens can inform nuanced treatment decisions. We evaluated effectiveness and identified predictors of SVR for ledipasvir/sofosbuvir +/- ribavirin (LDV/SOF +/-RBV) and ombitasvir/paritaprevir/ritonavir + dasabuvir (OPrD) +/-RBV in patients treated in routine practice. METHODS: Observational, intent-to-treat cohort of 21,142 genotype-1 patients initiating 8 or 12 weeks of LDV/SOF +/-RBV or 12 weeks of OPrD +/-RBV at any Veterans Affairs facility. Multivariate logistic regression models were constructed to model SVR and identify predictors. RESULTS: SVR was 91.2% (9,781/10,720) for LDV/SOF, 89.6% (3,266/3,646) for LDV/SOF+RBV, 91.7% (1,197/1,306) for OPrD and 87.8% (3,365/3,832) for OPrD+RBV. For LDV/SOF +/-RBV, reduced odds of SVR occurred in African-Americans (0.80, 95% CI 0.70, 0.92, P<0.001), body mass index (BMI)<25 (0.77, 95% CI 0.66, 0.90, P<0.001), BMI>/=30 (0.77, 95% CI 0.67, 0.89, P<0.001), proton pump inhibitors (PPIs; 0.81, 95% CI 0.71, 0.92, P<0.001), decompensated liver disease (0.58, 95% CI 0.45, 0.74, P<0.001) and FIB4>3.25 (0.60, 95% CI 0.53, 0.69, P<0.001). For OPrD +/-RBV, FIB-4>3.25 negatively predicted SVR (0.72, 95% CI 0.59, 0.88, P<0.001). Detectable 4-week on-treatment HCV RNA>/=15 IU/ml reduced SVR odds for both regimens (LDV/SOF +/-RBV OR 0.49, 95% CI 0.41, 0.58, P<0.001; OPrD +/-RBV OR 0.38, 95% CI 0.29, 0.50, P<0.001). Receipt of OPrD+RBV compared to LDV/SOF reduced odds of SVR (OR 0.70, 95% CI 0.62, 0.80, P<0.001). Mental health diagnosis did not impact likelihood of SVR. CONCLUSIONS: The diversity and size of this cohort allowed for extensive examination of regimen-specific predictors of SVR. FIB-4>3.25 and detectable 4-week on-treatment HCV RNA had the greatest negative impact. African-American race, low or high BMI, and PPIs negatively impacted odds of SVR for LDV/SOF +/-RBV. Mental health diagnoses did not.
Kinetic mechanism of protein arginine methyltransferase 6 (PRMT6).[Pubmed:22219200]
J Biol Chem. 2012 Feb 17;287(8):6062-71.
The protein arginine methyltransferases (PRMTs) are a family of enzymes that catalyze the mono- and dimethylation of arginine residues in a variety of proteins. Although these enzymes play important roles in a variety of cellular processes, aberrant PRMT activity is associated with several disease states, including heart disease and cancer. In an effort to guide the development of inhibitors targeting individual PRMTs, we initiated studies to characterize the molecular mechanisms of PRMT catalysis. Herein, we report studies on the kinetic mechanism of PRMT6. Initial velocity, product inhibition, and dead-end analog inhibition studies with the AcH4-21 and R1 peptides, as well as their monomethylated versions, indicate, in contrast to a previous report, that PRMT6 utilizes a rapid equilibrium random mechanism with dead-end EAP and EBQ complexes.
