YC 1 |
| Catalog No.GC16406 |
Lificiguat (YC-1) is a no-dependent soluble guanylyl cyclase(sGC) activator and a Hypoxia-inducible faction-1alpha (HIF-1alpha) inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 170632-47-0
Sample solution is provided at 25 µL, 10mM.
Lificiguat (YC-1) is a no-dependent soluble guanylyl cyclase(sGC) activator and a Hypoxia-inducible faction-1alpha (HIF-1alpha) inhibitor[1-3].
YC-1(0.01-100 µM;24/48 h) inhibits Wnt signaling and suppresses cell proliferation in hepatocellular carcinoma (HCC) [4]. Combination of sorafenib and YC-1(10 µmol/L; 48 h) synergistically inhibited proliferation and colony formation of HepG2, BEL-7402 and HCCLM3 cells[5]. The level of VEGF protein in YC-1 cell culture medium decreased in a dose-dependent manner compared with the VEGF protein level in medium from untreated cells grown under hypoxic conditions[6].
YC-1-treated(30 µg/g;i.p;2 weeks) mice tumors expressed lower levels of HIF-1α, less vascularization, and lower levels of HIF-1-inducing genes than control[6]. 10 mg/kg YC-1(i.p; every three days from day 7 after transplantation) significantly suppressed the growth of both 4T1 and MDA-MB-231 umors[7]. Sevoflurane postconditioning can provide neuroprotection after hypoxic-ischemic injury. Injection of 1.52 µg of the hypoxia-inducible factor-1α inhibitor YC-1 into the left lateral ventricle 30 minutes before hypoxic-ischemic injury reversed the neuroprotection induced by sevoflurane in mice[8].
References:
[1]. Martin E, Lee YC, et,al. YC-1 activation of human soluble guanylyl cyclase has both heme-dependent and heme-independent components. Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):12938-42. doi: 10.1073/pnas.231486198. Epub 2001 Oct 30. PMID: 11687640; PMCID: PMC60803.
[2]. Purohit R, Fritz BG, et,al. YC-1 binding to the β subunit of soluble guanylyl cyclase overcomes allosteric inhibition by the α subunit. Biochemistry. 2014 Jan 14;53(1):101-14. doi: 10.1021/bi4015133. Epub 2013 Dec 30. PMID: 24328155; PMCID: PMC3914721.
[3]. Nayak BK, Shanmugasundaram K, et,al. HIF-1 Mediates Renal Fibrosis in OVE26 Type 1 Diabetic Mice. Diabetes. 2016 May;65(5):1387-97. doi: 10.2337/db15-0519. Epub 2016 Feb 23. PMID: 26908870; PMCID: PMC4839204.
[4]. Wu JY, Shih YL, et,al. YC-1 Antagonizes Wnt/β-Catenin Signaling Through the EBP1 p42 Isoform in Hepatocellular Carcinoma. Cancers (Basel). 2019 May 13;11(5):661. doi: 10.3390/cancers11050661. PMID: 31086087; PMCID: PMC6562864.
[5]. Kong J, Kong F, et,al. YC-1 enhances the anti-tumor activity of sorafenib through inhibition of signal transducer and activator of transcription 3 (STAT3) in hepatocellular carcinoma. Mol Cancer. 2014 Jan 13;13:7. doi: 10.1186/1476-4598-13-7. PMID: 24418169; PMCID: PMC3895679.
[6]. Yeo EJ, Chun YS, et,al. YC-1: a potential anticancer drug targeting hypoxia-inducible factor 1. J Natl Cancer Inst. 2003 Apr 2;95(7):516-25. doi: 10.1093/jnci/95.7.516. PMID: 12671019.
[7]. Li Y, Zhang MZ, et,al. HIF-1α inhibitor YC-1 suppresses triple-negative breast cancer growth and angiogenesis by targeting PlGF/VEGFR1-induced macrophage polarization. Biomed Pharmacother. 2023 May;161:114423. doi: 10.1016/j.biopha.2023.114423. Epub 2023 Feb 21. PMID: 36822023.
[8]. Gao QS, Zhang YH, et,al. Brief inhalation of sevoflurane can reduce glial scar formation after hypoxic-ischemic brain injury in neonatal rats. Neural Regen Res. 2021 Jun;16(6):1052-1061. doi: 10.4103/1673-5374.300456. PMID: 33269750; PMCID: PMC8224129.
| Cell experiment [1]: | |
|
Cell lines |
Hep3B cells |
|
Preparation Method |
Cells were placed on a plate and then treated with YC-1 or DMSO for 5 minutes to determine VEGF levels in Normoxia or hypoxia. |
|
Reaction Conditions |
0.01-10µM YC-1；24h |
|
Applications |
The level of VEGF protein in YC-1 cell culture medium decreased in a dose-dependent manner compared with untreated cells grown under hypoxic conditions. |
| Animal experiment [2]: | |
|
Animal models |
Male nude (BALB/cAnNCrj-nu/nu) mice |
|
Preparation Method |
Mice(bearing carcinoma) received daily intraperitoneal injections of vehicle or YC-1 (30 microg/g) for 2 weeks. |
|
Dosage form |
30 µg/g YC-1; i.p;2 weeks |
|
Applications |
YC-1-treated mice tumors expressed lower levels of HIF-1α, less vascularization, and lower levels of HIF-1-inducing genes than control. |
|
References: [1]. Yeo EJ, Chun YS, et,al. YC-1: a potential anticancer drug targeting hypoxia-inducible factor 1. J Natl Cancer Inst. 2003 Apr 2;95(7):516-25. doi: 10.1093/jnci/95.7.516. PMID: 12671019. |
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| Cas No. | 170632-47-0 | SDF | |
| Chemical Name | (5-(1-benzyl-1H-indazol-3-yl)furan-2-yl)methanol | ||
| Canonical SMILES | OCC1=CC=C(C2=NN(CC3=CC=CC=C3)C4=CC=CC=C42)O1 | ||
| Formula | C19H16N2O2 | M.Wt | 304.34 |
| Solubility | ≥ 30.4mg/mL in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2858 mL | 16.429 mL | 32.858 mL |
| 5 mM | 0.6572 mL | 3.2858 mL | 6.5716 mL |
| 10 mM | 0.3286 mL | 1.6429 mL | 3.2858 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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