BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research[1][2].
IC50 & Target
IC50: 46.11 nM (LeuRS and RagD interaction)[1]Kd: 42.1 nM (LeuRS and RagD interaction)[1]
体外研究 (In Vitro)
BC-LI-0186 (0-20 μM; starved for 90 min in the leucine-free medium and then in the serum-free media for 15 min) inhibits phosphorylation of S6K in a dose- and time-dependent manner, but it has no effects on hosphorylation of AKT (S473)[1]. BC-LI-0186 (0-20 μM; 6 hours) induces cleaved poly (ADP-ribose) polymerase (PARP) and caspase-3 and an increase of p62 in A549 and H460 cells[1].BC-LI-0186 exhibits cytotoxic effect at nanomolar concentration in NSCLC cells, it exhibits IC50 values of 98 nM, 206 nM, 55 nM, 78 nM, 83 nM, 86 nM, 102 nM, 109 nM, 128 nM, and 206 nM in A549, H460, H2228, H1703, SNU1330, H1650, H2009, H358, H2279, H460, and H596 cells, respectively[1].BC-LI-0186 overcome acquired rapamycin resistance and inhibits the mTORC1 pathway in isogenic HCT116 cell lines that harbored either M TOR WT (HCT116 MW) or S2035I mutations (HCT116 MM), it exhibits little changed efficacy between the wild-type and mutant cells (GI50: 39.49 nM and 42.03 nM, EC50: 105.03 nM and 100.45 nM)[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.
Starved for 90 min in the leucine-free medium and then in the serum-free media for 15 min
Result:
Suppressed leucine-mediated mTORC1 activation in NSCLC cells.
体内研究 (In Vivo)
BC-LI-0186 (intraperitoneal injection; 50 mg/kg; alone or combines with cisplatin alone; 2 weeks; bid for 5 days per week) exhibits antitumor effects and significantly reduces tumor size compared with treatment with vehicle in an LSL K-ras G12D lung cancer animal model[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:
K-ras mouse lung cancer modelan LSL K-ras G12D lung cancer animal model[1]
Dosage:
50 mg/kg
Administration:
Intraperitoneal injection; 50 mg/kg; alone or combines with cisplatin alone; 2 weeks; bid for 5 days per week
Result:
Showed activated caspase-3-positive cells higher in the BC-LI-0186-treated group than in the vehicle or cisplatin-treated group.Reduced p-S6 and p-AKT level whereas cisplatin alone has minimal effect on both p-S6 and p-AKT expression.Showed a slight (not statistically significant) increase in body weight during the treatment period.Exhibited a specific inhibition of mTORC1 and not mTORC2.
分子量
429.53
Formula
C22H27N3O4S
CAS 号
695207-56-8
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Jong Hyun Kim, et al. Control of leucine-dependent mTORC1 pathway through chemical intervention of leucyl-tRNA synthetase and RagD interaction. Nat Commun. 2017 Sep 29;8(1):732.
R-BC154 acetate is a selective fluorescent α9β1 integrin antagonist. R-BC154 acetate acts as a useful high affinity, activation dependent integrin probe, which can be used to investigate α9β1 and α4β1 integrin binding activity[1].
IC50 & Target[1]
α9β1
体外研究 (In Vitro)
R-BC154 acetate has 3 times greater affinities for α9β1 (Ki=12.7 nM) relative to α4β1 (Ki=38.0 nM) under Ca2+/Mg2+ conditions in human glioblastoma LN18 cell lines[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
R-BC154 acetate (10 mg/kg; i.v.) acts as an in vivo probe for bone marrow haemopoietic stem cells in mice[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
C57Bl/6 mice (6-8 weeks old)[1]
Dosage:
10 mg/kg
Administration:
Intravenous injection
Result:
Was capable of binding haemopoietic progenitor cells and HSC within mice bone marrow in vivo.
分子量
1184.36
Formula
C56H65N9O14S3
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]. Design, synthesis and binding properties of a fluorescent α9β1/α4β1 integrin antagonist and its application as an in vivo probe for bone marrow haemopoietic stem cells. Org Biomol Chem. 2014 Feb 14;12(6):965-78.
R-BC154 acetate is a selective fluorescent α9β1 integrin antagonist. R-BC154 acetate acts as a useful high affinity, activation dependent integrin probe, which can be used to investigate α9β1 and α4β1 integrin binding activity[1].
IC50 & Target[1]
α9β1
体外研究 (In Vitro)
R-BC154 acetate has 3 times greater affinities for α9β1 (Ki=12.7 nM) relative to α4β1 (Ki=38.0 nM) under Ca2+/Mg2+ conditions in human glioblastoma LN18 cell lines[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.
体内研究 (In Vivo)
R-BC154 acetate (10 mg/kg; i.v.) acts as an in vivo probe for bone marrow haemopoietic stem cells in 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:
C57Bl/6 mice (6-8 weeks old)[1]
Dosage:
10 mg/kg
Administration:
Intravenous injection
Result:
Was capable of binding haemopoietic progenitor cells and HSC within mice bone marrow in vivo.
分子量
1184.36
Formula
C56H65N9O14S3
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]. Design, synthesis and binding properties of a fluorescent α9β1/α4β1 integrin antagonist and its application as an in vivo probe for bone marrow haemopoietic stem cells. Org Biomol Chem. 2014 Feb 14;12(6):965-78.
R-BC154 acetate is a selective fluorescent α9β1 integrin antagonist. R-BC154 acetate acts as a useful high affinity, activation dependent integrin probe, which can be used to investigate α9β1 and α4β1 integrin binding activity[1].
IC50 & Target[1]
α9β1
体外研究 (In Vitro)
R-BC154 acetate has 3 times greater affinities for α9β1 (Ki=12.7 nM) relative to α4β1 (Ki=38.0 nM) under Ca2+/Mg2+ conditions in human glioblastoma LN18 cell lines[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
R-BC154 acetate (10 mg/kg; i.v.) acts as an in vivo probe for bone marrow haemopoietic stem cells in mice[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
C57Bl/6 mice (6-8 weeks old)[1]
Dosage:
10 mg/kg
Administration:
Intravenous injection
Result:
Was capable of binding haemopoietic progenitor cells and HSC within mice bone marrow in vivo.
分子量
1184.36
Formula
C56H65N9O14S3
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]. Design, synthesis and binding properties of a fluorescent α9β1/α4β1 integrin antagonist and its application as an in vivo probe for bone marrow haemopoietic stem cells. Org Biomol Chem. 2014 Feb 14;12(6):965-78.
