GLPBio

YC 1

Catalog No.: GC16406Purity:>99.00%
Lificiguat (YC-1) is a no-dependent soluble guanylyl cyclase(sGC) activator and a Hypoxia-inducible faction-1alpha (HIF-1alpha) inhibitor.

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YC 1
Cas No.: 170632-47-0
10mM (in 1mL DMSO)In Stock
$43.00
1
5mgIn Stock
$38.00
1
10mgIn Stock
$54.00
1
50mgIn Stock
$196.00
1
100mgIn Stock
$350.00
1
200mgIn Stock
$560.00
1

Citations

1 publicationsPublications from researchers using this product

Description

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.

Protocol

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.

Product Documents

Purity:>99.00%Appearance:A solid

Chemical Properties

CAS No.
170632-47-0
Chemical Name
(5-(1-benzyl-1H-indazol-3-yl)furan-2-yl)methanol
SMILES
OCC1=CC=C(C2=NN(CC3=CC=CC=C3)C4=CC=CC=C42)O1
Molecular Formula
C19H16N2O2
Molecular Weight
304.34
Solubility
≥ 30.4mg/mL in DMSO
Storage
Store at RT
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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