FR901464 is a potent spliceosome inhibitor with prominent anti-tumor and anti-cancer effects[1].
体外研究 (In Vitro)
FR901464 (10-20 ng/ml; 6-24 hours) inhibits the growth of murine solid tumors, Colon 38 carcinoma and Meth A fibrosarcoma. FR901464 induces characteristic G1 and G2/M phase arrest in the cell cycle and internucleosomal degradation of genomic DNA with the same kinetics as activation of SV40 promoter-dependent cellular transcription in M-8 tumor cells[1].FR901464 (1-10 ng/ml; 16 hours) suppresses the transcription of some inducible endogenous genes but not house keeping genes in M-8 cells[1].FR901464 exhibits potent anticancer activity. It shows enhancement of activity of a promoter of the SV40 DNA tumor virus at 10 nM concentration in M-8 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
507.62
Formula
C27H41NO8
CAS 号
146478-72-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. II. Activities against experimental tumors in mice and mechanism of action. J Antibiot (Tokyo). 1996 Dec;49(12):1204-11.
[2]. Arun K Ghosh, et al. Enantioselective total syntheses of FR901464 and spliceostatin A and evaluation of splicing activity of key derivatives. J Org Chem. 2014 Jun 20;79(12):5697-709.
FR 900098 Monosodium Salt is a member of a unique class of phosphonic acid natural products that inhibit the nonmevalonate pathway for isoprenoid biosynthesis.
FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC50s of 0.51 μM (Ki=0.31 μM) and 0.33 μM (Ki=0.14 μM), respectively[1].
IC50 & Target[1]
ERK1
0.31 μM (Ki)
ERK2
0.14 μM (Ki)
ERK2
0.33 μM (IC50)
ERK1
0.51 μM (IC50)
体外研究 (In Vitro)
In AP-1-transfected cells, FR180204 dose-dependently inhibits AP-1 transactivation with IC50 of 3.1 μM[1]. FR 180204 inhibits spontaneous mesothelioma cell growth[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.
体内研究 (In Vivo)
FR180204 (100 mg/kg, i.p., b.i.d.) significantly decreases the severity of symptoms and body weight loss in collagen-induced arthritis mice[2]. In a mouse model of dengue virus (DENV) infection, FR180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves clinical parameters[4].
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
327.34
Formula
C18H13N7
CAS 号
865362-74-9
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Ohori M, et al. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem Biophys Res Commun. 2005 Oct 14;336(1):357-63.
[2]. Ohori M, et al. FR180204, a novel and selective inhibitor of extracellular signal-regulated kinase, ameliorates collagen-induced arthritis in mice. Naunyn Schmiedebergs Arch Pharmacol. 2007 Jan;374(4):311-6.
[3]. Honda M, et al. Mesothelioma cell proliferation through autocrine activation of PDGF-ββ receptor. Cell Physiol Biochem. 2012;29(5-6):667-74
[4]. Sreekanth GP, et al. Role of ERK1/2 signaling in dengue virus-induced liver injury. Virus Res. 2014 Aug 8;188:15-26
Kinase Assay [1]
Nunc-Immuno MaxiSorp plates are coated with 20 μg/mL MBP solution in phosphate-buffered saline (PBS). After washing with PBS containing 0.05% Tween 20 (T-PBS), blocking buffer (T-PBS containing 3% BSA) is added to each well and the plates are incubated for 10 min at room temperature. After washing with T-PBS, chemical compounds, ATP and recombinant ERK2 diluted in assay dilution buffer (20 mM Mops, pH 7.2, 25 mM β-glycerol phosphate, 5 mM EGTA, 1 mM sodium orthovanadate, 1 mM dithiothreitol, and 50 μg/mL BSA) and are added to each well. Vehicle groups (containing 0.1% DMSO) and kinase-withdrawal groups are used for the control and basal determinations. After incubation for 1 h at room temperature, plates are washed twice with T-PBS. Anti-phospho MBP antibody (0.2 μg/mL) is added to each well, and the plates are incubated for 1 h at room temperature. After washing, anti-mouse HRP-conjugated polyclonal antibodies are added and the plates are incubated for 30 min.
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.
Animal Administration [2]
In brief, mice are randomized and grouped by body weight immediately before treatment. Bovine CII is dissolved in 0.1mol/Lacetic acid at the concentration of 10 mg/mL and then emulsified in an equal volume of Freund’s complete adjuvant H37Rv. Apart from a naive group, each mouse is immunized with 25 μL of the CII emulsion into the tail base, followed by a boost injection 3 weeks after primary injection (day 0). FR180204 and methylprednisolone are ground and suspended in 0.1% methylcellulose solution to a volume of 5 mL/kg. Drugs are given by twice daily intraperitoneal injection from days 0 to 12 in accordance with pharmacokinetic studies with superior area under the curve and Cmax values of i.p. versus s.c. or p.o. administration. The initial administration is 30 min before the boost CII injection. The clinical score of arthritis is obtained by summing the visual severity grade of each limb, scored as follows: 0, no arthritis; 1, one swollen digit; 2, two or more swollen digits or swelling of the entire paw without ankylosis; 3, gross swelling with ankylosis of the paw. Body weight is measured on day 12.
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]. Ohori M, et al. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem Biophys Res Commun. 2005 Oct 14;336(1):357-63.
[2]. Ohori M, et al. FR180204, a novel and selective inhibitor of extracellular signal-regulated kinase, ameliorates collagen-induced arthritis in mice. Naunyn Schmiedebergs Arch Pharmacol. 2007 Jan;374(4):311-6.
[3]. Honda M, et al. Mesothelioma cell proliferation through autocrine activation of PDGF-ββ receptor. Cell Physiol Biochem. 2012;29(5-6):667-74
[4]. Sreekanth GP, et al. Role of ERK1/2 signaling in dengue virus-induced liver injury. Virus Res. 2014 Aug 8;188:15-26
[1]. Francesca Ricciardiello, et al. Inhibition of the Hexosamine Biosynthetic Pathway by Targeting PGM3 Causes Breast Cancer Growth Arrest and Apoptosis. Cell Death Dis. 2018 Mar 7;9(3):377.
FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect[1].
体外研究 (In Vitro)
FR054 (0.5-1 mM, 24-48 h) induces an early proliferation arrest followed by a marked cell death increase in breast cancer cells and induces apoptosis. The effect of FR054 occurs through PGM3 inhibition instead of other off-target effects[1]. FR054 (250 μM, 24 h) treatment efficiently affects both N- and O-glycosylation levels in MDA-MB-231 cells[1]. FR054 induces endoplasmic reticulum (ER) stress and a ROS-dependent apoptotic cell death[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.
Cell Viability Assay[1]
Cell Line:
MDA-MB-231 cells.
Concentration:
0.5-1 mM.
Incubation Time:
48 h.
Result:
Reduced viability and a significant increase of the apoptosis as compared to the control clone.
体内研究 (In Vivo)
FR054 (1000 mg/kg, ip) suppresses cancer growth in MDA-MB-231 xenograft mice[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.
Animal Model:
Mice were subcutaneously injected with MDA-MB-231 cells[1].
Dosage:
1000 mg/kg.
Administration:
IP, single or fractionated dose (twice a day 500 mg/kg/dose).
Result:
Appears to have an in vivo antitumor efficacy that is higher when administered twice a day compared to single administration.
分子量
329.30
Formula
C14H19NO8
CAS 号
35954-65-5
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Francesca Ricciardiello, et al. Inhibition of the Hexosamine Biosynthetic Pathway by targeting PGM3 causes breast cancer growth arrest and apoptosis. Cell Death Dis. 2018 Mar 7;9(3):377.
FR901463 是一种有效的抗癌试剂 (anti-cancer agent),可用于癌症研究。FR901463 增强 SV40 DNA 病毒启动子的转录活性。
FR901463 Chemical Structure
CAS No. : 146478-74-2
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
FR901463 is a potent anti-cancer agent and can be used for cancer research. FR901463 enhances the transcriptional activity of the promoter of SV40 DNA virus[1].
分子量
544.08
Formula
C27H42ClNO8
CAS 号
146478-74-2
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]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities. J Antibiot (Tokyo). 1996 Dec;49(12):1196-203.
FR901465 is a potent anti-cancer and anti-tumor agent. FR901465 can be used for cancer research[1].
体外研究 (In Vitro)
FR901465 prolongs the life of mice bearing murine ascitic tumor P388 leukemia (T/C values 127% for FR901465 in mice bearing murine ascitic tumors[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
523.62
Formula
C27H41NO9
CAS 号
146478-73-1
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]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. II. Activities against experimental tumors in mice and mechanism of action. J Antibiot (Tokyo). 1996 Dec;49(12):1204-11.
[2]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. III. Structures of FR901463, FR901464 and FR901465. J Antibiot (Tokyo). 1997 Jan;50(1):96-9.
[3]. Ratnakar N. Asolkar, et al. Discovery and Development of Natural Products for Pest Management. RETURN TO BOOKPREVCHAPTERNEXT
FR901463 是一种有效的抗癌试剂 (anti-cancer agent),可用于癌症研究。FR901463 增强 SV40 DNA 病毒启动子的转录活性。
FR901463 Chemical Structure
CAS No. : 146478-74-2
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
FR901463 is a potent anti-cancer agent and can be used for cancer research. FR901463 enhances the transcriptional activity of the promoter of SV40 DNA virus[1].
分子量
544.08
Formula
C27H42ClNO8
CAS 号
146478-74-2
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]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities. J Antibiot (Tokyo). 1996 Dec;49(12):1196-203.
FR901463 是一种有效的抗癌试剂 (anti-cancer agent),可用于癌症研究。FR901463 增强 SV40 DNA 病毒启动子的转录活性。
FR901463 Chemical Structure
CAS No. : 146478-74-2
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
FR901463 is a potent anti-cancer agent and can be used for cancer research. FR901463 enhances the transcriptional activity of the promoter of SV40 DNA virus[1].
分子量
544.08
Formula
C27H42ClNO8
CAS 号
146478-74-2
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]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities. J Antibiot (Tokyo). 1996 Dec;49(12):1196-203.
FR901465 is a potent anti-cancer and anti-tumor agent. FR901465 can be used for cancer research[1].
体外研究 (In Vitro)
FR901465 prolongs the life of mice bearing murine ascitic tumor P388 leukemia (T/C values 127% for FR901465 in mice bearing murine ascitic tumors[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
523.62
Formula
C27H41NO9
CAS 号
146478-73-1
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]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. II. Activities against experimental tumors in mice and mechanism of action. J Antibiot (Tokyo). 1996 Dec;49(12):1204-11.
[2]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. III. Structures of FR901463, FR901464 and FR901465. J Antibiot (Tokyo). 1997 Jan;50(1):96-9.
[3]. Ratnakar N. Asolkar, et al. Discovery and Development of Natural Products for Pest Management. RETURN TO BOOKPREVCHAPTERNEXT
FR901465 is a potent anti-cancer and anti-tumor agent. FR901465 can be used for cancer research[1].
体外研究 (In Vitro)
FR901465 prolongs the life of mice bearing murine ascitic tumor P388 leukemia (T/C values 127% for FR901465 in mice bearing murine ascitic tumors[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
523.62
Formula
C27H41NO9
CAS 号
146478-73-1
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]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. II. Activities against experimental tumors in mice and mechanism of action. J Antibiot (Tokyo). 1996 Dec;49(12):1204-11.
[2]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. III. Structures of FR901463, FR901464 and FR901465. J Antibiot (Tokyo). 1997 Jan;50(1):96-9.
[3]. Ratnakar N. Asolkar, et al. Discovery and Development of Natural Products for Pest Management. RETURN TO BOOKPREVCHAPTERNEXT