AM-Imidazole-PA-Boc is an alkyl chain-based PROTAC linker can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966)[1].
IC50 & Target
Alkyl-Chain
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
254.33
Formula
C12H22N4O2
CAS 号
2357108-99-5
运输条件
Room temperature in continental US; may vary elsewhere.
Heliotrine N-oxide 是 Heliotrine (HY-126128) 对应的吡咯利嗪生物碱类氮氧化物 (PA N-oxide)。Heliotrine N-oxide 可导致吡咯基 DNA 加合物 (DNA adduct) 的形成,并可能引发 PA 诱导的肝肿瘤的启动。
Heliotrine N-oxide Chemical Structure
CAS No. : 6209-65-0
规格
是否有货
100 mg
询价
250 mg
询价
500 mg
询价
* Please select Quantity before adding items.
生物活性
Heliotrine N-oxide is the corresponding PA (pyrrolizidine alkaloid) N-oxide of Heliotrine (HY-126128). Heliotrine N-oxide leads to the formation of pyrrolic DNA adducts and potential initiation of PA-induced liver tumors in vivo[1].
体外研究 (In Vitro)
DNA adduct is a segment of DNA bound to a cancer-causing chemical. This process could be the start of a cancerous cell, or carcinogenesis.
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
329.39
Formula
C16H27NO6
CAS 号
6209-65-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Xiaobo He, et al. Pyrrolizidine alkaloid-derived DNA adducts are common toxicological biomarkers of pyrrolizidine alkaloid N-oxides. J Food Drug Anal. 2017 Oct;25(4):984-991.
Heliotrine N-oxide 是 Heliotrine (HY-126128) 对应的吡咯利嗪生物碱类氮氧化物 (PA N-oxide)。Heliotrine N-oxide 可导致吡咯基 DNA 加合物 (DNA adduct) 的形成,并可能引发 PA 诱导的肝肿瘤的启动。
Heliotrine N-oxide Chemical Structure
CAS No. : 6209-65-0
规格
是否有货
100 mg
询价
250 mg
询价
500 mg
询价
* Please select Quantity before adding items.
生物活性
Heliotrine N-oxide is the corresponding PA (pyrrolizidine alkaloid) N-oxide of Heliotrine (HY-126128). Heliotrine N-oxide leads to the formation of pyrrolic DNA adducts and potential initiation of PA-induced liver tumors in vivo[1].
体外研究 (In Vitro)
DNA adduct is a segment of DNA bound to a cancer-causing chemical. This process could be the start of a cancerous cell, or carcinogenesis.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
329.39
Formula
C16H27NO6
CAS 号
6209-65-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Xiaobo He, et al. Pyrrolizidine alkaloid-derived DNA adducts are common toxicological biomarkers of pyrrolizidine alkaloid N-oxides. J Food Drug Anal. 2017 Oct;25(4):984-991.
Heliotrine N-oxide 是 Heliotrine (HY-126128) 对应的吡咯利嗪生物碱类氮氧化物 (PA N-oxide)。Heliotrine N-oxide 可导致吡咯基 DNA 加合物 (DNA adduct) 的形成,并可能引发 PA 诱导的肝肿瘤的启动。
Heliotrine N-oxide Chemical Structure
CAS No. : 6209-65-0
规格
是否有货
100 mg
询价
250 mg
询价
500 mg
询价
* Please select Quantity before adding items.
生物活性
Heliotrine N-oxide is the corresponding PA (pyrrolizidine alkaloid) N-oxide of Heliotrine (HY-126128). Heliotrine N-oxide leads to the formation of pyrrolic DNA adducts and potential initiation of PA-induced liver tumors in vivo[1].
体外研究 (In Vitro)
DNA adduct is a segment of DNA bound to a cancer-causing chemical. This process could be the start of a cancerous cell, or carcinogenesis.
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
329.39
Formula
C16H27NO6
CAS 号
6209-65-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Xiaobo He, et al. Pyrrolizidine alkaloid-derived DNA adducts are common toxicological biomarkers of pyrrolizidine alkaloid N-oxides. J Food Drug Anal. 2017 Oct;25(4):984-991.
(+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM.
IC50 & Target
10.4 nM (BET)[1].
体外研究 (In Vitro)
(+)-JQ1 PA is a derivative of JQ1, which is the inhibitor of BET. The IC50 of (+)-JQ1 PA for BET is 10.4 nM, and the IC50 of JQ1 is 14.3 nM in MV4;11 cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
437.95
Formula
C22H20ClN5OS
CAS 号
2115701-93-2
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Tyler DS, et al. Click chemistry enables preclinical evaluation of targeted epigenetic therapies. Science. 2017 Jun 30;356(6345):1397-1401.
Cell Assay [1]
Proliferation of MV4;11 cells after 72 hours of treatment, comparing JQ1 versus JQ1-PA are tested. Cell cycle profile of MV4;11 cells after 48 hours of treatment with DMSO, JQ1, JQ1-PA, or JQ1-TCO (all compounds used at 500 nM) are tested[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Tyler DS, et al. Click chemistry enables preclinical evaluation of targeted epigenetic therapies. Science. 2017 Jun 30;356(6345):1397-1401.
Pretomanid-d4 (PA-824-d4) is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 µg/mL[1][2].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
363.28
Formula
C14H8D4F3N3O5
CAS 号
1346617-34-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Stover CK, et al. A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. Nature. 2000 Jun 22;405(6789):962-6.
[3]. Lenaerts AJ, et al. Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models. Antimicrob Agents Chemother. 2005 Jun;49(6):2294-301.
[4]. Manjunatha UH, et al. Mycobacterium leprae is naturally resistant to PA-824. Antimicrob Agents Chemother. 2006 Oct;50(10):3350-4.
Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 µg/mL[1].
IC50 & Target
Tuberculosis.
体外研究 (In Vitro)
Pretomanid (PA-824) exhibited a sub-micromolar minimal inhibitory concentration (MIC) against MTB, Although Pretomanid (PA-824) was not the most potent NAP against cultured MTB clinical isolates, it was the most active in infected mice when orally administered at 25 mg/kg. This indicated that Pretomanid (PA-824) might possess more desirable pharmacokinetic properties than the other more potent NAP compounds that we tested. Further studies in mice at 25, 50 and 100 mg kg-1 Pretomanid (PA-824) daily for 10 days resulted in reductions of mycobacterial burden in both spleen and lung tissues that were comparable to that of INH at 25 mg kg -1 [1]. Pretomanid (PA-824) showed significant activity at 2, 10, and 50 microg/ml, similar to that of metronidazole, in a dose-dependent manner. Pretomanid (PA-824) at 100 mg/kg in cyclodextrin/lecithin was as active as moxifloxacin at 100 mg/kg and isoniazid at 25 mg/kg and was slightly more active than rifampin at 20 mg/kg. Long-term treatment with Pretomanid (PA-824) at 100 mg/kg in cyclodextrin/lecithin reduced the bacterial load below 500 CFU in the lungs and spleen [2]. Pretomanid (PA-824) has no effect on the viability of M. leprae in all three models, consistent with the lack of the nitroimidazo-oxazine-specific nitroreductase, encoded by Rv3547 in the M. leprae genome, which is essential for activation of this molecule [3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
359.26
Formula
C14H12F3N3O5
CAS 号
187235-37-6
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Stover CK, et al. A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. Nature. 2000 Jun 22;405(6789):962-6.
[2]. Lenaerts AJ, et al. Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models. Antimicrob Agents Chemother. 2005 Jun;49(6):2294-301.
[3]. Manjunatha UH, et al. Mycobacterium leprae is naturally resistant to PA-824. Antimicrob Agents Chemother. 2006 Oct;50(10):3350-4.
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity[1].
IC50 & Target
IC50: 28.2 nM (BRD4 BD1) and 7.2 nM (BRD4 BD2)[1]
体外研究 (In Vitro)
CD161 (NKR-P1A) has Kis of 8.2 nM and 1.4 nM for BRD4 BD1 and BRD4 BD2, respectively[1]. CD161 (30-3000 nM; 1 hours) is very effective in inducing rapid down-regulation of c-Myc at as early as the 1 h time point and in a dose-dependent manner[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[1]
Cell Line:
MV4;11 leukemia cells.
Concentration:
30, 100, 300, 1000, 3000 nM
Incubation Time:
1 hours
Result:
Induced rapid down-regulation of c-Myc at as early as the 1 hours time point and in a dose-dependent manner.
体内研究 (In Vivo)
CD161 (NKR-P1A) (po; 20, 40 mg/kg/day; 45 days) achieves essentially complete tumor growth inhibition[1]. CD161 (5 mg/kg (iv), 25 mg/kg (po); 0-24 hours) has the t1/2 of 2.4 hours (iv) and 2.9 hours (po) for rat; the Cmax of 7333 ng/mL (po) for rat. The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) [1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Dorsal side of severe combined immunodeficient (SCID) mice[1]
5 mg/kg (iv), 25 mg/kg (po) for rat and mice (Pharmacokinetic Study)
Administration:
Iv and po; 0, 5, 15, 30 mins, and 1, 2, 4, 6, 8, 24 hours
Result:
The t1/2 of rat is 2.4 hours (iv) and 2.9 hours (po); the Cmaxof rat is 7333 ng/mL (po). The t1/2 of mice is 0.5 hours (iv) and 1.60 hours (po); the Cmax of mice is 983.1 ng/mL (po) [1].
分子量
435.48
Formula
C26H21N5O2
CAS 号
1627716-22-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Zhao Y, et al. Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor. J Med Chem. 2017 May 11;60(9):3887-3901.