Name: Lificiguat (YC-1)
Brand: Selleck Chemicals
SKU: S7958
Availability: InStock
Rating: 5 (36 reviews)

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Quality Control

Batch: Purity: 99.94%

99.94

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src FLT FLT3 HER2 Bcr-Abl
Other HIF Inhibitors	PT2399 PX-478 Dihydrochloride BAY 87-2243 KC7F2 IOX2 CAY10585 (LW 6) PT2385 Molidustat (BAY 85-3934) IDF-11774 MK-8617

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 61 mg/mL (200.43 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 31 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.050mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 61 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.510mg/ml (1.68mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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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.

Chemical Information, Storage & Stability

Molecular Weight	304.34	Formula	C₁₉H₁₆N₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	170632-47-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=N2)C4=CC=C(O4)CO

Mechanism of Action

Targets/IC₅₀/Ki	sGC HIF-1α
In vitro	Lificiguat (YC-1) is an allosteric activator of soluble guanylyl cyclase (sGC). It increases the catalytic rate of the enzyme and sensitizes the enzyme toward its gaseous activators nitric oxide or carbon monoxide. This compound 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 . 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 are likely to be linked with the oxygen-sensing pathway and not with the activation of soluble guanylyl cyclase.
In vivo	Administration of Lificiguat (YC-1) to experimental animals results in the inhibition of platelet-rich thrombosis and a decrease of mean arterial pressure, which correlates with increased cGMP levels . This compound 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 its anti-platelet aggregation effect does not appear to affect tumor growth .
References	[1] https://pubmed.ncbi.nlm.nih.gov/11687640/ [2] https://pubmed.ncbi.nlm.nih.gov/12671019/

Applications

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

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Lificiguat (YC-1) HIF inhibitor

Chemical Structure

Molecular Weight: 304.34