Lificiguat(YC-1)

Catalog No.S7958

Lificiguat(YC-1) Chemical Structure

Molecular Weight(MW): 304.34

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

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Biological Activity

Description 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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A498 cells NY\qfIx6S3m2b4TvfIlkcXS7IHHzd4F6 MVq0PEBp M1nHdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1QThiY3XscJMhcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuN{DPxE1? NYi2cG5LOjZ{M{W5OVE>
ACHN cells MXfGeY5kfGmxbjDhd5NigQ>? MY[0PEBp NFHNOI1CdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBR2hPKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYm= NU\Yc4ZOOjByOUe0OVY>
HeLa cells NXPNfmdHTnWwY4Tpc44h[XO|YYm= M1f3N2lvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKEiLRkHhcJBp[SC2cnHud4NzcXC2aX;uZYwh[WO2aY\peJkhcW5iaIXtZY4hUGWOYTDj[YxteyCneIDy[ZN{cW6pIFjSSU1NfWNiYX\0[ZIhOTJiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OD1zLkWg{txO M1:xTlI1QTByNk[y
NCI-H226 cells NVjZZoFLTnWwY4Tpc44h[XO|YYm= MUi0PEBp MmflRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOjZiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlkh|ryP NI\IeW4zODB7N{S1Oi=>
AGS cells M1XFbGZ2dmO2aX;uJIF{e2G7 MorhTY5pcWKrdHnvckBw\iCqeYDvfIliKGmwZIXj[YQhUEmIMTD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gbJVu[W5iQVfTJINmdGy|IHL5JINmdGxvYnHz[YQhUFKHIILldI9zfGW{IHHzd4F6NCCLQ{WwQVIh|ryP MVexO|MzQDV|Mh?=
HepG2 cells MUfDfZRwfG:6aXPpeJkh[XO|YYm= MoXpO|IhcA>? NEXjc2FEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVIvOiEQvF2= MnTqNlQ6ODB4NkK=
HCT116 cells NVjZdmRXS3m2b4TvfIlkcXS7IHHzd4F6 MlToO|IhcA>? NHOzTnREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0zNjJizszN NIexN48zPDlyME[2Ni=>
HEK293 cells M4fHNmZ2dmO2aX;uJIF{e2G7 M1fl[FE3KGh? M{HlSGlvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKEiLRkHhcJBp[SC2cnHud4NzcXC2aX;uZYwh[WO2aY\peJkhcW5iSFXLNlk{KGOnbHzzJIlv[3WkYYTl[EBnd3JiMU[gbJJ{KGK7IHj5dI95cWFicnXzdI9ve2ViZXzlcYVvfC2mcnn2[Y4hdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxRTlwMkGg{txO NF3OW2YyQTR|NU[2NS=>
Hep3B cells NHPRXIlHfW6ldHnvckBie3OjeR?= M4Xjd2lvcGmkaYTpc44hd2ZiaInwc5hq[SCrbnT1Z4VlKEiLRkGtZYxxcGFidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGmwIHj1cYFvKEincEPCJINmdGy|IHL5JJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NVMvQCEQvF2= NUnFeVZQOTd6OES0PVU>
U251HRE cells Ml\2SpVv[3Srb36gZZN{[Xl? NW\5[YlLUW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRiSFnGNUBi[3SrdnH0bY9vKGmwIHj1cYFvKFV{NUHIVmUh[2WubIOgZpkh[2WubDDiZZNm\CC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDJR|UxRTF2Lkig{txO Mk\iNVg2ODF4MEG=
HL60 cells MUnDfZRwfG:6aXPpeJkh[XO|YYm= M4P2UVQ5KGh? MmfwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUK1MlI4KM7:TR?= M4fON|I{QDNzOEC5
HT1080 cells MXPGeY5kfGmxbjDhd5NigQ>? NEL5WnlKdmirYnn0bY9vKG:oIFjJSlEhcW5iaIXtZY4hUFRzMEiwJINmdGy|IITyZY5{\mWldHXkJJdqfGhiNYjIVmUweEeOMz;WSWdHN0VzYjDy[ZBwenSncjDwcIF{dWmmIIDy[U1qdmO3YnH0[YQh\m:{IEGgbJIh\m:ubH;3[YQh[nliaX7jeYJifGmxbjD1coRmeiCqeYDvfIliKGOxbnTpeIlwdnNiZn;yJFI1KGi{czDifUBJWkVvZILpeoVvKGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OD12OD60JO69VQ>? MoPMNlU4PzNyMUS=

... Click to View More Cell Line Experimental Data

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].

Protocol

Cell Research:[2]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Male nude (BALB/cAnNCrj–nu/nu) mice
  • Formulation: DMSO
  • Dosages: 30 µg/g
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 60 mg/mL (197.14 mM)
Ethanol 60 mg/mL (197.14 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 304.34
Formula

C19H16N2O2

CAS No. 170632-47-0
Storage powder
Synonyms N/A

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HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID