1346753-00-1
1346753-00-1
Chemical Structure
YHO-13351
- CAS No.: 1346753-00-1
- Formula:C27H37N3O7S2
- Molecular Weight:579.73
IUPAC Name: (Z)-1-(5-(2-cyano-2-(3,4-dimethoxyphenyl)vinyl)thiophen-2-yl)piperidin-4-yl diethylglycinate methanesulfonate
InChIKey: XOEIHKAPFXUACW-QMGGKDRNSA-N
SMILES: N#C/C(C1=CC=C(OC)C(OC)=C1)=C\C2=CC=C(N3CCC(OC(CN(CC)CC)=O)CC3)S2.O=S(C)(O)=O
Biological Activity: YHO-13351 is an orally active ABCG2 inhibitor. YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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YHO-13351 | 98.07% | YHO-13351 is an orally active ABCG2 inhibitor. YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer. | ||||||||||||||||||||
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FLLL32 | 99.41% | FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells. | ||||||||||||||||||||
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Pacrinolol | Pacrinolol (HOE 224) is a selective and orally active beta1 adrenergic receptor blocker. Pacrinolol can inhibit Isoprenaline (HY-108353)-induced positive inotropic effect and increased heart rate. Pacrinolol can be used for the research of cardiovascular disease. | |||||||||||||||||||||
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YHO-13177 | 99.65% | YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model. | ||||||||||||||||||||
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YHO-13351 free base | 98.42% | YHO-13351 free base is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP. | ||||||||||||||||||||
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Zatebradine hydrochloride (Standard) | ≥98% | Zatebradine (hydrochloride) (Standard) is the analytical standard of Zatebradine (hydrochloride). This product is intended for research and analytical applications. Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 μM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 μM, 2.21 μM, 1.90 μM and 1.88 μM, respectively. | ||||||||||||||||||||
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TML-6 | 98.08% | TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research. | ||||||||||||||||||||
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iNOS-IN-2 | iNOS-IN-2 (Compound 53) is a potent down-regulator of inducible nitric oxide synthase (iNOS) protein. iNOS-IN-2 effectively inhibits the NO production (IC50=6.4 μM). iNOS-IN-2 has a potential therapeutic effect on chronic inflammation. | |||||||||||||||||||||
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Antitumor agent-155 | Antitumor agent-155 (Compound 13) inhibits microtubule polymerization, induces autophagy and apoptosis. Antitumor agent-155 shows cytotoxicity against HCT116, A549, AGS, SK-MES-1 cells with IC50s of 0.227, 0.253, 0.574, 0.423 μM respectively. | |||||||||||||||||||||
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Mebeverine hydrochloride (Standard) | ≥98% | Mebeverine (hydrochloride) (Standard) is the analytical standard of Mebeverine (hydrochloride). This product is intended for research and analytical applications. Mebeverine hydrochloride, a β-phenylethylamine derivative, is a musculotropic agent that potently blocks intestinal peristalsis. Mebeverine directly blocks voltage-operated sodium channels and inhibits intracellular calcium accumulation. | ||||||||||||||||||||
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Dimethomorph (Standard) | ≥98% | Dimethomorph (Standard) is the analytical standard of Dimethomorph. This product is intended for research and analytical applications. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 µM. | ||||||||||||||||||||
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References
- [1]. Chang CH, et al. Combining ABCG2 Inhibitors with IMMU-132, an Anti-Trop-2 Antibody Conjugate of SN-38, Overcomes Resistance to SN-38 in Breast and Gastric Cancers. Mol Cancer Ther. 2016;15(8):1910-1919. [Content Brief]
- [2]. Yamazaki R, et al. Novel acrylonitrile derivatives, YHO-13177 and YHO-13351, reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo. Mol Cancer Ther. 2011;10(7):1252-1263. [Content Brief]
- [3]. Shishido Y, et al. ABCG2 inhibitor YHO-13351 sensitizes cancer stem/initiating-like side population cells to irinotecan. Anticancer Res. 2013;33(4):1379-1386. [Content Brief]
