IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3[1]. IPAG induces apoptosis[2].
体外研究 (In Vitro)
Sigma1 inhibition by IPAG causes the autolysosomal degradation of PD-L1 in PC3 (hormone-insensitive prostate cancer) and MDA-MB-231 (triple-negative breast cancer) cell lines and reduces the levels of functional PD-L1 on the surface of the cells[2]. IPAG treatment produces a mean of 100±8 μg per 106 cells. IPAG can inhibit cell proliferation. Treatment with IPAG decreases cell mass[3]. IPAG treatment suppresses phosphorylation of translational regulator proteins p70S6K, S6, and 4E-BP1[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[3]
Cell Line:
T47D cells
Concentration:
10 μM
Incubation Time:
24 hours
Result:
The mean forward scatter height (FSC-H) of DMSO (control) measured 412±5, whereas the mean FSC-H of IPAG treated cells was 390±4.
Western Blot Analysis[3]
Cell Line:
T47D cells
Concentration:
10 μM
Incubation Time:
Result:
Decreased levels of phospho-threonine 389-p70S6Kinase (P-S6K), phospho-serine 235/236-ribosomal S6 (P-S6), and phospho-serine 65-4E-BP1 (P-4E-BP1).
分子量
395.28
Formula
C17H22IN3
CAS 号
193527-91-2
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]. James M Brimson, et al. Simple ammonium salts acting on sigma-1 receptors yield potential treatments for cancer and depression. Sci Rep. 2020 Jun 8;10(1):9251.
[2]. Halley M Oyer, et al.Small-Molecule Modulators of Sigma1 and Sigma2/TMEM97 in the Context of Cancer: Foundational Concepts and Emerging Themes. Front Pharmacol. 2019 Oct 21;10:1141.
[3]. Felix J Kim, et al. Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression. Biochem Biophys Res Commun. 2012 Sep 21;426(2):177-82.
FEN1-IN-2 (compound 20) is a flap endonuclease 1 (FEN1) inhibitor, with IC50 values of 3 nM and 226 nM for FEN1 and XPG, respectively[1].
IC50 & Target
IC50: 3 nM (FEN1), 226 nM (XPG)[1].
分子量
393.42
Formula
C20H15N3O4S
CAS 号
824983-94-0
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]. L Nathan Tumey, et al. The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors. Bioorg Med Chem Lett. 2005 Jan 17;15(2):277-81.
Amine functionalized silica nanoparticles or micro beads from Nanocs have narrow size distribution yet with multiple size selection from 5 nm to 50 microns. Amine groups on these silica beads can be used to react with a number of functional groups such as succinimidy NHS ester, COOH and many other groups. Nanocs functional silica nanoparticle or micro beads are suspended in 1% aqeuous solution. Standard deviation of these silica particles is in the range of 10% of listed size parameter. Nanocs also offers various fluorescently labeled and surface functionalized silica particles for wide biomedical research and bioassay development. These surface modified silica particles provide our customers with more choices for in-vitro or in-vivo applications of those nanoparticles. Customer conjugation and modification is available upon request.
Product specifications:
1% suspension in aqueous solution, other concentration available upon request;
Particle shape: Spherical;
Surface functionality: Primary amine (-NH2);
Appearance: Clear or translucent color depends on particle size;
13-Methyltetradecanoic acid (13-MTD), a saturated branched-chain fatty acid with potent anticancer effects. 13-Methyltetradecanoic acid induces apoptosis in many types of human cancer cells[1][2].
体外研究 (In Vitro)
13-Methyltetradecanoic acid (13-MTD; 0-140 μg/mL; 12-24 hours) inhibits cell viability and proliferation in human bladder cancer cells by inducing apoptosis[1]. 13-Methyltetradecanoic acid (13-MTD; 70 μg/mL; 2-48 hours) treatments results in significant accumulation of cells with sub-G1 DNA content in a time-dependent manner, with the proportion of sub-G1 phase DNA content ranging from 9.25% to 85.3% over 2-48 hours[1]. 13-Methyltetradecanoic acid (13-MTD; 70 μg/mL; 2-24 hours) down-regulates Bcl-2 and up-regulates Bax. This promotes mitochondrial dysfunction, leading to the release of cytochrome c from the mitochondria to the cytoplasm, as well as the proteolytic activation of caspases. 13-Methyltetradecanoic acid down-regulates AKT phosphorylation and activates phosphorylation of p38 and c-Jun N-terminal kinase (JNK)[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.
Inhibition of cell viability in a dose- and time-dependent manner.
Cell Cycle Analysis[1]
Cell Line:
Bladder cancer cell lines T24, 5637, and UM-UC-3
Concentration:
70 μg/mL
Incubation Time:
2 hours, 8 hours, 24 hours, or 48 hours
Result:
Resulted in significant accumulation of cells with sub-G1 DNA content in a time-dependent manner.
Western Blot Analysis[1]
Cell Line:
T24, 5637, and UM-UC-3 cells
Concentration:
70 μg/mL
Incubation Time:
2 hours, 8 hours, 24 hours
Result:
Down-regulated Bcl-2 and up-regulated Bax, and down-regulated AKT phosphorylation and activated phosphorylation of p38 and c-Jun N-terminal kinase (JNK).
体内研究 (In Vivo)
13-Methyltetradecanoic acid (13-MTD; 70 mg/kg/day; oral gavage; daily; for 30 days) significantly suppresses tumor growth in a xenograft model[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 Model:
BALB/C nude mice injected with Jurkat lymphoma cells[2]
Dosage:
70 mg/kg/day
Administration:
Oral gavage; daily; for 30 days
Result:
Effectively inhibited the growth in vivo in a xenograft model.
分子量
242.40
Formula
C15H30O2
CAS 号
2485-71-4
中文名称
13-甲基十四烷酸
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]. Tianxin Lin, et al. 13-Methyltetradecanoic acid induces mitochondrial-mediated apoptosis in human bladder cancer cells. Urol Oncol. May-Jun 2012;30(3):339-45.
[2]. Qingqing Cai, et al. 13-methyltetradecanoic acid exhibits anti-tumor activity on T-cell lymphomas in vitro and in vivo by down-regulating p-AKT and activating caspase-3. PLoS One. 2013 Jun 7;8(6):e65308.
VPC-18005 抑制 ERG 诱导的转录,并直接与 ERG-ETS 结构域结合,并破坏 ERG 与 DNA 的结合。VPC-18005是一种荧光素酶活性的有效抑制剂。
VPC-18005 Chemical Structure
CAS No. : 2242480-48-2
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
VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity[1].
体外研究 (In Vitro)
VPC-18005 is found to inhibit pETS-luc reporter activity in PNT1B-ERG and VCaP cells with IC50 values of 3 and 6 μM, respectively[1]. VPC-18005 could suppress ERG reporter activity without exhibiting overt cytotoxicity[1]. VPC-18005 inhibits migration and invasion of ERG-overexpressing cells in vitro[1]. VPC-18005 can antagonize the metastatic potential of ERG-expressing prostate cells[1]. The exposure of larvae to 1 or 10 µM of VPC-18005 produced a 20–30% decrease in the dissemination of cancer cells in zebrafsh[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
PNT1B-Mock cells and PNT1B-ERG cells.
Concentration:
5 µM.
Incubation Time:
24 h.
Result:
Inhibited migration and invasion of prostate cell lines in vitro.
分子量
319.38
Formula
C15H17N3O3S
CAS 号
2242480-48-2
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]. Miriam S Butler, et al. Discovery and characterization of small molecules targeting the DNA-binding ETS domain of ERG in prostate cancer. Oncotarget. 2017 Jun 27;8(26):42438-42454.
[2]. Haneen Amawi, et al. The use of zebrafish model in prostate cancer therapeutic development and discovery. Cancer Chemother Pharmacol. 2021 Mar;87(3):311-325.
cis-Tiliroside, a kaempferol derivative, is a flavonoid glycoside. cis-Tiliroside exhibits better cytotoxic activity than trans-Tiliroside in A549 cell line[1].
体外研究 (In Vitro)
cis-Tiliroside has CC50s of 68.05 μg/mL and 18.82 μg/mL for A549 cell line in 24 h or 48 h, respectively. trans-Tiliroside has CC50s of 149.90 μg/mL and 144.74 μg/mL for A549 cell line in 24 h or 48 h, respectively[1]. cis-Tiliroside exhibits better cytotoxic activity than kaempferol, which has CC50s of 129.15 μg/mL and 113.48 μg/mL for A549 cell line in 24 h or 48 h, respectively[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
594.52
Formula
C30H26O13
CAS 号
163956-16-9
中文名称
顺式银椴苷
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]. Chi-Ren Liao, et al. Studies on cytotoxic constituents from the leaves of Elaeagnus oldhamii Maxim. in non-small cell lung cancer A549 cells. Molecules. 2014 Jul 4;19(7):9515-34.
Thalidomide-5-methyl is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein[1].
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].
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
272.26
Formula
C14H12N2O4
CAS 号
40313-92-6
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]. George W. Muller, et al. Substituted 2-(2,6 dioxo-3-fluoropiperidin-3-yl)-isoindolines and method of reducing TNFα levels. Patent US5874448A.
Galectin-3 is a β Galactoside specific carbohydrate recognition protein (lectin) has the ability to promote the migration of B cell precursor acute lymphoblastic leukemia (BCP-ALL) cells and withstand drug therapy.
分子量
461.42
Formula
C22H23NO10
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]. Bum-Erdene K,et al. Novel Selective Galectin-3 Antagonists Are Cytotoxic to Acute Lymphoblastic Leukemia. J Med Chem. 2022 Apr 28;65(8):5975-5989.