Home Angiogenesis HIF inhibitor - Guanylate Cyclase inhibitor Lificiguat (YC-1) For research use only.

Lificiguat (YC-1)

Lificiguat (YC-1) is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).

Lificiguat (YC-1) Chemical Structure

Lificiguat (YC-1) Chemical Structure

CAS No. 170632-47-0

Purity & Quality Control

Lificiguat (YC-1) Related Products

Signaling Pathway

HIF Signaling Pathways

HIF Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf21 Function assay Activation of sGC Enzyme (soluble Guanylate Cyclase) in Sf21 cells infected with baculo virus in the presence of 30 nM of PAPA/NO, EC50 = 4.11 μM. 11141091
HL60 Cytotoxicity assay Cytotoxicity against HL60 cells by Propidium iodide exclusion assay, ED50 = 25.27 μM. 17189698
HT60 Apoptosis assay 26 uM 48 hrs Induction of apoptosis in HT60 cells at 26 uM after 48 hrs 17189698
AGS Function assay Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells by cell-based HRE reporter assay, IC50 = 2 μM. 17328532
Hep3B Function assay Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay, IC50 = 13.8 μM. 17328532
AGS Function assay Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS cells by reporter gene assay, IC50 = 2 μM. 17884495
Hep3B Function assay Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay, IC50 = 13.8 μM. 17884495
U251HRE Function assay Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay, IC50 = 14.8 μM. 18501601
HEK293 Function assay 16 hrs Inhibition of hypoxia-induced HIF1alpha transcriptional activity in HEK293 cells incubated for 16 hrs by hypoxia response element-driven luciferase reporter gene assay, IC50 = 9.21 μM. 19435661
HeLa Function assay 30 uM 4 hrs Inhibition of HIF1alpha accumulation in human HeLa cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot 19435661
HCT116 Function assay 30 uM 4 hrs Inhibition of HIF1alpha accumulation in human HCT116 cells at 30 uM incubated for 4 hrs under hypoxic conditions by Western blot 19435661
ACHN Antitumor assay 48 hrs Antitumor activity against human ACHN cells after 48 hrs by MTT assay, IC50 = 0.3 μM. 20097456
NCI-H226 Antitumor assay 48 hrs Antitumor activity against human NCI-H226 cells after 48 hrs by MTT assay, IC50 = 1.9 μM. 20097456
A498 Cytotoxicity assay 48 hrs Cytotoxicity against human A498 cells after 48 hrs by MTT assay, IC50 = 0.37 μM. 23831809
HL60 Cytotoxicity assay 48 hrs Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50 = 25.27 μM. 23831809
HeLa Function assay 12 hrs Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay, IC50 = 1.5 μM. 24900662
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 2.2 μM. 24900662
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2.2 μM. 24900662
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50 = 29.3 μM. 24900662
HT1080 Proliferation assay 72 hrs Inhibition of cell proliferation of human HT1080 cells after 72 hrs by WST-8 dye based cell counting assay, IC50 = 30.9 μM. 25773014
HT1080 Function assay 1 hr Inhibition of HIF1 in human HT1080 cells transfected with 5xHRE/pGL3/VEGF/E1b reporter plasmid pre-incubated for 1 hr followed by incubation under hypoxia conditions for 24 hrs by HRE-driven luciferase reporter gene assay, IC50 = 48.4 μM. 25773014
A498 Cytotoxicity assay 48 hrs Cytotoxicity against human A498 cells incubated for 48 hrs by MTT assay, IC50 = 0.3 μM. 26235951
HL60 Cytotoxicity assay 48 hrs Cytotoxicity against human HL60 cells incubated for 48 hrs by MTT assay, IC50 = 25.27 μM. 26235951
A498 Cytotoxicity assay 48 hrs Cytotoxicity against human A498 cells after 48 hrs by MTT assay, IC50 = 0.3 μM. 26820553
HL60 Cytotoxicity assay 48 hrs Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50 = 25.3 μM. 26820553
HCT116 Function assay 3 uM Reduction of insulin-induced HIF-1 alpha expression in human HCT116 cells at 3 uM by western blot analysis 27157007
HeLa Function assay 12 hrs Inhibition of hypoxia-induced HIF1 transcriptional activity in human HeLa cells measured after 12 hrs by luciferase reporter gene assay, IC50 = 1.2 μM. 27847273
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RXF631L Growth inhibition assay Growth inhibition of human RXF631L cells by SRB assay, GI50 = 0.15849 μM. ChEMBL
NCI-H226 Growth inhibition assay Growth inhibition of human NCI-H226 cells by SRB assay, GI50 = 0.22387 μM. ChEMBL
RXF631L Growth inhibition assay Growth inhibition of human RXF631L cells by SRB assay, TGI = 0.52481 μM. ChEMBL
NCI-H226 Growth inhibition assay Growth inhibition of human NCI-H226 cells by SRB assay, TGI = 0.66069 μM. ChEMBL
HeLa Function assay 12 hrs Inhibition of HIF-1 (unknown origin) expressed in human HeLa cells after 12 hrs by HRE luciferase reporter gene assay, IC50 = 2 μM. ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description Lificiguat (YC-1) is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).
Targets
sGC [1] HIF-1α [2]
In vitro
In vitro YC-1 is an allosteric activator of soluble guanylyl cyclase (sGC). YC-1 increases the catalytic rate of the enzyme and sensitizes the enzyme toward its gaseous activators nitric oxide or carbon monoxide. YC-1 alone activates the enzyme only 10-fold, but it potentiates the CO- and NO-dependent activation of sGC, resulting in stimulation of the highly purified enzyme that may be several hundred- to several thousand-fold [1]. It inhibits platelet aggregation and vascular contraction and also inhibits HIF-1 activity in vitro. YC-1 completely blocks HIF-1α expression at the post-transcriptional level and consequently inhibits the transcription factor activity of HIF-1 in hepatoma cells cultured under hypoxic conditions, suggesting that these effects of YC-1 are likely to be linked with the oxygen-sensing pathway and not with the activation of soluble guanylyl cyclase[2].
Cell Research Cell lines Hep3B cells
Concentrations 0.01-10 μM
Incubation Time 24 h
Method Hep3B cells are plated in a six-well plate at a density of 1 × 105 cells/well in α-modified Eagle medium supplemented with 10% heat-inactivated FBS and incubated overnight. Cells are treated with YC-1 (0.01-10 μM) or vehicle (DMSO) for 5 minutes and are then subjected to normoxia or hypoxia for 24 hours. VEGF levels in the conditioned media are quantified by using the Quantikine human VEGF Immunoassay kit. The VEGF concentrations are quantified by comparison with a series of VEGF standard samples included in the assay kit.
Experimental Result Images Methods Biomarkers Images PMID
Western blot HO-1 / HO-2 HIF-1α p-ERK / p-p38 MAPK / p-JNK1 / p-AKT EZH2 / EZH1 / H3K27me3 / Histone H3 DNMT1 / DNMT3a / DNMT3b 18923065
Growth inhibition assay Cell proliferation Cell viability 22507221
In Vivo
In vivo The administration of YC-1 to experimental animals results in the inhibition of the platelet-rich thrombosis and a decrease of the mean arterial pressure, which correlates with increased cGMP levels [1]. YC-1 effectively inhibits tumor growth in tumor-bearing mice. The inhibition of HIF-1 activity in tumors from YC-1-treated mice is associated with blocked angiogenesis and an inhibition of tumor growth, while the anti-platelet aggregation effect of YC-1 does not appear to affect tumor growt[2].
Animal Research Animal Models Male nude (BALB/cAnNCrj–nu/nu) mice
Dosages 30 µg/g
Administration i.p.

Chemical Information & Solubility

Molecular Weight 304.34 Formula

C19H16N2O2
CAS No. 170632-47-0 SDF Download Lificiguat (YC-1) SDF
Smiles C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=N2)C4=CC=C(O4)CO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 61 mg/mL ( (200.43 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 31 mg/mL

Water : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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