(E)-Akt inhibitor-IV ((E)-AKTIV) is a PI3K-Akt inhibitor, with potent cytotoxic[1].
IC50 & Target
Akt[1]
体外研究 (In Vitro)
(E)-Akt inhibitor-IV (compound 7) exhibits average GI20 of 0.04 μM on four cell lines (MDA-MB468 cells, MDA-MB231 cells, MCF7 cells and 184B5 cells)[1]. (E)-Akt inhibitor-IV shows little effects on the growth of 184B5 non-cancer cells at the average GI20 doses[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
614.54
Formula
C31H27IN4S
CAS 号
959841-49-7
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]. Changkun Hu, et al. A 4-aminoquinoline derivative that markedly sensitizes tumor cell killing by Akt inhibitors with a minimum cytotoxicity to non-cancer cells. Eur J Med Chem. 2010 Feb;45(2):705-9.
Polygalacin D (PGD) 是从桔梗 Platycodon grandiflorum 中分离的具有抗癌和抗增殖特性的生物活性化合物。 Polygalacin D 抑制 IAP 蛋白家族的表达,包括存活蛋白,cIAP-1 和 cIAP-2 蛋白,并通过抑制 GSK3β,Akt 的磷酸化和PI3K 的表达来阻断 PI3K/Akt 途径。Polygalacin D 通过 PI3K/Akt 途径诱导凋亡 (apoptosis)。
Polygalacin D Chemical Structure
CAS No. : 66663-91-0
规格
价格
是否有货
数量
1 mg
¥1520
In-stock
5 mg
¥4570
In-stock
10 mg
询价
50 mg
询价
* Please select Quantity before adding items.
Polygalacin D 相关产品
•相关化合物库:
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Apoptosis Compound Library
Natural Product Library
Anti-Cancer Compound Library
Glycoside Compound Library
Medicine Food Homology Compound Library
Terpenoids Library
Traditional Chinese Medicine Monomer Library
生物活性
Polygalacin D (PGD) is a bioactive compound isolated from Platycodon grandiflorum (Jacq.) with anticancer and anti-proliferative properties. PGD suppresses the expression of the IAP family of proteins including survivin, cIAP-1 and cIAP-2 and blocks the PI3K/Akt pathway by inhibiting the phosphorylation of GSK3β, Akt and the expression of PI3K. Polygalacin D induces apoptosis[1]
IC50 & Target
IC50: IAP[1]
体外研究 (In Vitro)
Polygalacin D (0-40 µM; 48 hours) inhibits cell proliferation with IC50s of 26.49 µM in the A549 cells and 20.52 µM in the H460 cells[1]. Polygalacin D (0-20 µM; 48 hours) increases the proportion of early and late apoptotic cells, and nuclear condensation is observed in A549 and H460 cells[1]. Polygalacin D (0-20 µM; 48 hours) may exerts its apoptotic effects by regulating the apoptotic proteins and the IAP family of proteins in A549 and H460 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.
Cell Proliferation Assay[1]
Cell Line:
A549 and H460 cancer cell lines
Concentration:
10 µM, 20 µM, 40µM
Incubation Time:
48 hours
Result:
Inhibited the proliferation of NSCLC cell lines.
Apoptosis Analysis[1]
Cell Line:
A549 and H460 cancer cell lines
Concentration:
10 µM, 20 µM
Incubation Time:
48 hours
Result:
Induced apoptosis of NSCLC cell lines.
Western Blot Analysis[1]
Cell Line:
A549 and H460 cancer cell lines
Concentration:
10 µM, 20 µM
Incubation Time:
48 hours
Result:
Decreased survivin, c-IAP-1 and c-IAP-2 expression.
分子量
1209.32
Formula
C57H92O27
CAS 号
66663-91-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Seo YS, et al. Polygalacin D induces apoptosis and cell cycle arrest via the PI3K/Akt pathway in non-small cell lung cancer. Oncol Rep. 2018 Apr;39(4):1702-1710.
AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
IC50 & Target
IC50: 1.042 μM (AKT)[1]
体外研究 (In Vitro)
AKT-IN-1 is able to potently inhibit phosphorylation of AKT in cells at both Thr308 and Ser473, with IC50s of 0.422 and 0.322 μM, respectively. AKT-IN-1 inhibits the phosphorylation of ribosomal protein S6, a downstream effector of the PI3K-AKT pathway. AKT-IN-1 potently inhibits the phosphorylation of PRAS40[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)
The effects of AKT-IN-1 (Compound 26) in vivo are characterized by measuring the pharmacodynamic activity of AKT-IN-1 in a BT474c breast adenocarcinoma xenograft model. Following acute doses of 100 and 200 mg/kg, AKT-IN-1 potently inhibits the phosphorylation of its downstream substrate GSK3β as well as the phosphorylation of AKT (Ser473), with a potency consistent with its pharmacokinetic profile. The in vivo activity of AKT-IN-1 is further characterized by measuring the effects on the growth of tumor cell xenografts. Continuous (daily) oral dosing of AKT-IN-1 (100 and 200 mg/kg) to nude mice bearing BT474c breast adenocarcinoma xenografts results in inhibition of tumor growth in a dose-dependent manner. When dosed at 200 mg/kg daily, AKT-IN-1 causes significant tumor growth inhibition[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
343.42
Formula
C22H21N3O
CAS 号
1357158-81-6
运输条件
Room temperature in continental US; may vary elsewhere.
PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
IC50 & Target[1]
PKBα
0.5 nM (IC50)
PKA
450 nM (IC50)
体外研究 (In Vitro)
PF-AKT400 (Compound 42) provides significantly enhanced selectivity for Akt relative to earlier leads such as spiroindoline 2. Free IC50 and EC50 values are estimated for phospho-S6 reduction (110 nM) and Akt hyperphosphorylation (216 nM), respectively. These values corresponded well to the cellular IC50 for PF-AKT400 in U87 cells measuring p-GSK-3α (310 nM)[2].
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)
PF-AKT400 is subsequently evaluated for modulation of Akt in tumors and in multiple in vivo mouse models of antitumor efficacy. It is active in a PC3 prostate carcinoma xenograft experiment, with 75% TGI observed at 100 mg/kg b.i.d. dosing for 10 days. In a colorectal carcinoma (Colo205) xenograft study, PF-AKT400 produces 60% TGI at 150 mg/kg b.i.d. after 10 days. Most intriguingly, in combination with Rapamycin (10 mg/kg, ip), 75 mg/kg b.i.d. (10 days) of PF-AKT400 results in 98% TGI in an additional PC3 prostate carcinoma xenograft study compared to 56% TGI and 66% TGI with PF-AKT400 and Rapamycin as single agents. To define the in vivo potency of PF-AKT400 (Compound 42) in the PC3 xenograft model, oral administration of 25, 75, and 100 mg/kg PF-AKT400 is performed with blood and tumor sampling over time. Immunoblot analysis of detergent-soluble extracts derived from PC3 tumors shows a significant reduction of S6 phosphorylation, and hyperphosphorylation of Akt upon treatment at doses that produced significant tumor growth inhibition. Plasma drug concentrations peak rapidly after oral administration of doses between 25-100 mg/kg (Tmax=0.5 h). Peak PD responses of phospho-S6 and phospho-Akt are observed at approximately 2-4h and 1h post-administration of PF-AKT400, respectively. The time-course of PD marker response is well described by a PK/PD model at doses that ranged from no efficacy (25 mg/kg) to maximal efficacy (100 mg/kg)[2].
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
400.43
Formula
C20H22F2N6O
CAS 号
1004990-28-6
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Chen SF, et al. Binding selectivity studies of PKBα using molecular dynamics simulation and free energy calculations. J Mol Model. 2013 Nov;19(11):5097-5112.
[2]. Freeman-Cook KD, et al. Design of selective, ATP-competitive inhibitors of Akt. J Med Chem. 2010 Jun 24;53(12):4615-4622.
Kinase Assay [2]
A fluorescence polarization IMAP type assay is used. An amount of 15 μL of diluted PF-AKT400 (Compound 42) in DMSO is mixed with 60 μL of reaction buffer (10 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.01% Triton-X100, 1 mM DTT). Then 5 μL of the compound/buffer mixture, 10 μL of a solution containing 4 μM ATP and 40 nM fluorescent-labeled Crosstide (Tamara-labeled GRPRTSSFAEG peptide), and 5 μL of Akt1 protein (lacking the pleckstrin homology (PH) domain, containing an Asp at position 473, and prephosphorylated at Thr 308) in reaction buffer are combined. After a 90 min incubation, IMAP beads are added and plates are read (lamp filter, 544 nm; emission filter, 615 nm). The same procedure can be applied to full length Akt1 to provide similar results. All IC50 values are the geometric mean of at least n=2 determinations[2].
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]
Mice[2] Studies to describe the PK/PD relationship for PF-AKT400 are performed in male SCID/Beige mice bearing subcutaneous PC3 prostate carcinoma xenografts. Once tumors reach about ~300mm3 in size, PF-AKT400 is formulated in 0.5% methylcellulose vehicle and administered orally to 3 mice per dose group. Plasma and tumors are harvested over time, tumor lysates prepared, and the levels of phospho S6 reduction and phospho Akt induction are evaluated by immunoblot.
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]. Chen SF, et al. Binding selectivity studies of PKBα using molecular dynamics simulation and free energy calculations. J Mol Model. 2013 Nov;19(11):5097-5112.
[2]. Freeman-Cook KD, et al. Design of selective, ATP-competitive inhibitors of Akt. J Med Chem. 2010 Jun 24;53(12):4615-4622.
AKT-IN-6 (Example 13) is a potent Akt inhibitor. AKT-IN-6 inhibits Akt1, Akt2 and Akt3 with IC50s < 500nM, respectively. (patent WO2013056015A1).
IC50 & Target
Akt1
Akt2
Akt3
体外研究 (In Vitro)
Akt is a central node in cell signaling downstream of growth factors, cytokines, and other cellular stimuli. Aberrant loss or gain of Akt activation underlies the pathophysiological properties of a variety of complex diseases, including type-2 diabetes and cancer[2].
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
389.43
Formula
C22H20FN5O
CAS 号
1430056-54-4
运输条件
Room temperature in continental US; may vary elsewhere.
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells[1].
IC50 & Target[1]
Akt1
1.4 nM (IC50)
Akt2
1.2 nM (IC50)
Akt3
1.7 nM (IC50)
PKA
0.3 nM (IC50)
P70S6K
8.9 (IC50)
分子量
526.36
Formula
C23H23Cl2F2N5O3
CAS 号
2374740-21-1
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]. Dong X, et al. Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design. J Med Chem. 2019 Aug 8;62(15):7264-7288.
AKT-IN-11 is one of the most effective antibacterial agents against human hepatoma BEL-7402 cell line with an IC50 value of 1.15μM.
IC50 & Target
AKT,ERK
1.15 μM (IC50)
分子量
521.96
Formula
C27H27ClF3NO4
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]. Hai Y,et al. Semisynthesis and biological evaluation of (+)-sclerotiorin derivatives as antitumor agents for the treatment of hepatocellular carcinoma. Eur J Med Chem. 2022 Feb 5;232:114166.
AKT-IN-11 is one of the most effective antibacterial agents against human hepatoma BEL-7402 cell line with an IC50 value of 1.15μM.
IC50 & Target
AKT,ERK
1.15 μM (IC50)
分子量
521.96
Formula
C27H27ClF3NO4
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]. Hai Y,et al. Semisynthesis and biological evaluation of (+)-sclerotiorin derivatives as antitumor agents for the treatment of hepatocellular carcinoma. Eur J Med Chem. 2022 Feb 5;232:114166.
AKT-IN-11 is one of the most effective antibacterial agents against human hepatoma BEL-7402 cell line with an IC50 value of 1.15μM.
IC50 & Target
AKT,ERK
1.15 μM (IC50)
分子量
521.96
Formula
C27H27ClF3NO4
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]. Hai Y,et al. Semisynthesis and biological evaluation of (+)-sclerotiorin derivatives as antitumor agents for the treatment of hepatocellular carcinoma. Eur J Med Chem. 2022 Feb 5;232:114166.
APN/AKT-IN-1 is a potent and dual inhibitor of APN and AKT with IC50s of 0.21 and 0.27 μM, respectively. APN/AKT-IN-1 can effectively inhibit the phosphorylation of GSK3β, the intracellular substrate of AKT[1].
分子量
389.45
Formula
C18H27N7O3
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]. Liu Q, et al. Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors. ACS Med Chem Lett. 2021;12(12):1932-1941.
APN/AKT-IN-1 is a potent and dual inhibitor of APN and AKT with IC50s of 0.21 and 0.27 μM, respectively. APN/AKT-IN-1 can effectively inhibit the phosphorylation of GSK3β, the intracellular substrate of AKT[1].
分子量
389.45
Formula
C18H27N7O3
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]. Liu Q, et al. Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors. ACS Med Chem Lett. 2021;12(12):1932-1941.
APN/AKT-IN-1 is a potent and dual inhibitor of APN and AKT with IC50s of 0.21 and 0.27 μM, respectively. APN/AKT-IN-1 can effectively inhibit the phosphorylation of GSK3β, the intracellular substrate of AKT[1].
分子量
389.45
Formula
C18H27N7O3
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]. Liu Q, et al. Design, Synthesis, and Biological Evaluation of APN and AKT Dual-Target Inhibitors. ACS Med Chem Lett. 2021;12(12):1932-1941.
AKT-IN-9 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-9 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 1)[1].
IC50 & Target
AKT[1]
分子量
452.98
Formula
C24H29ClN6O
CAS 号
2709045-53-2
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]. Xin Li, et al. Thickened dicyclic derivatives, their preparation methods and their application in medicine. Patent WO2021185238A1.
AKT-IN-10 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-10 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 4)[1].
IC50 & Target
AKT[1]
分子量
484.03
Formula
C26H34ClN5O2
CAS 号
2709045-56-5
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]. Xin Li, et al. Thickened dicyclic derivatives, their preparation methods and their application in medicine. Patent WO2021185238A1.
AKT-IN-9 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-9 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 1)[1].
IC50 & Target
AKT[1]
分子量
452.98
Formula
C24H29ClN6O
CAS 号
2709045-53-2
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]. Xin Li, et al. Thickened dicyclic derivatives, their preparation methods and their application in medicine. Patent WO2021185238A1.
AKT-IN-10 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-10 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 4)[1].
IC50 & Target
AKT[1]
分子量
484.03
Formula
C26H34ClN5O2
CAS 号
2709045-56-5
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]. Xin Li, et al. Thickened dicyclic derivatives, their preparation methods and their application in medicine. Patent WO2021185238A1.
AKT-IN-9 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-9 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 1)[1].
IC50 & Target
AKT[1]
分子量
452.98
Formula
C24H29ClN6O
CAS 号
2709045-53-2
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]. Xin Li, et al. Thickened dicyclic derivatives, their preparation methods and their application in medicine. Patent WO2021185238A1.