170632-47-0 Usage
Description
YC-1 (170632-47-0) is a nitric oxide-independent activator of soluble guanylyl cyclase (sGC). Significantly elevates cGMP levels and inhibits collagen-stimulated aggregation of rabbit platelets (IC50?= 14.6 μM).1?Induces human endometrial cancer cell senescence via modulation of HIF1α activity.2?Induces degradation of HIF1α.3?Protects against glutamate-induced neuronal damage4?and β-amyloid-induced toxicity in differentiated PC12 cells5.
Uses
YC-1 has been used as a hypoxia-inducible factor 1α (HIF-1α) inhibitor:to reduce hypoxia induced Jagged1 expression in cardiomyocytes (CMs)to study its effect on progenitor expansion and CD34+ and side population (SP) cell phenotype and on the proliferation rate of cells with an ability to form long term colony forming unitsto study its effect on regulating sphingosine 1-phosphate (S1P) bound to albumin induced plasminogen activator inhibitor 1 (PAI-1) expression by activating Rho/ Rho-associated protein kinase (ROCK) pathway.
General Description
A nitric oxide-independent, superoxide-sensitive activator of soluble guanylyl cyclase. Inhibits platelet adhesion to collagen and acts as an antithrombotic agent. Reported to reduce HIF-1α levels and xenograft growth.
Biochem/physiol Actions
YC-1 activates soluble guanylyl cyclase and prevents platelet aggregation and vascular contraction. It has a potential to treat circulation disorders. YC-1 also has an ability to inhibit hypoxia-inducible factor 1α (HIF-1α) activity in vitro. It acts as a potential antiangiogenic anticancer agent.
References
1) Martin?et al.?(2001),?YC-1 activation of human soluble guanylyl cyclase has both heme-dependent and heme-independent components;?Proc. Natl. Acad. Sci. USA,?98?12938
2) Kato?et al.?(2006),?Induction of human endometrial cancer cell senescence through modulation of HIF-1alpha activity by EGLN1; Int. J. Cancer,?118?1144
3) Kim?et al.?(2006),?A domain responsible for HIF-1alpha degradation by YC-1, a novel anticancer agent; Int. J. Oncol.,?29?255
4) Tai?et al. (2018),?Therapeutic window for YC-1 following glutamate-induced neuronal damage and transient focal cerebral ischemia; Mol. Med. Rep.,?17?6490
5) Tsai?et al.?(2013),?The role of heat shock protein 70 in the protective effect of YC-1 on β-amyloid-induced toxicity in differentiated PC12 cells.; PLoS One,?8(7)?e69320
Check Digit Verification of cas no
The CAS Registry Mumber 170632-47-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,7,0,6,3 and 2 respectively; the second part has 2 digits, 4 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 170632-47:
(8*1)+(7*7)+(6*0)+(5*6)+(4*3)+(3*2)+(2*4)+(1*7)=120
120 % 10 = 0
So 170632-47-0 is a valid CAS Registry Number.
170632-47-0Relevant articles and documents
Hypoxia-Targeting Organometallic Ru(II)-Arene Complexes with Enhanced Anticancer Activity in Hypoxic Cancer Cells
Zhao, Jian,Li, Wanchun,Gou, Shaohua,Li, Shuang,Lin, Shengqiu,Wei, Qianhui,Xu, Gang
, p. 8396 - 8403 (2018)
As hypoxia is an important factor to limit chemotherapeutic efficacy in tumors, we herein report three ruthenium(II)-arene complexes containing a hypoxia inducible factor-1α inhibitor (YC-1), which endow the organometallic complexes with potential for hyp
Palladium-Catalyzed C-H/C-H Cross-Coupling by Mechanochemistry: Direct Alkenylation and Heteroarylation of N1-Protected 1 H-Indazoles
Yu, Jingbo,Yang, Xinjie,Wu, Chongyang,Su, Weike
, p. 1009 - 1021 (2020/01/09)
C3-alkenylated and C3-(hetero)arylated 1H-indazoles are privileged structural motifs in numerous pharmaceuticals. Direct C3-alkenylation and C3-(hetero)arylation of 1H-indazoles have been significantly challenging because of the inert nature of this carbon center. Herein, we present an efficient mechanochemical strategy for palladium-catalyzed C-H/C-H cross-coupling to construct C3-alkenylated and C3-heteroarylated 1H-indazoles using low-cost copper oxidants with satisfactory product yields and broad functional group tolerance. The robustness of the developed protocols was further demonstrated by the unprecedented total mechanosynthesis of the intermediate of PLK4 inhibitor CFI-400945 and HIF-1α inhibitor YC-1.
Copper(I) Oxide-Mediated Cyclization of o-Haloaryl N-Tosylhydrazones: Efficient Synthesis of Indazoles
Tang, Meng,Kong, Yuanfang,Chu, Bingjie,Feng, Dan
supporting information, p. 926 - 939 (2016/04/05)
An efficient synthesis of indazoles from readily accessible E/Z mixtures of o-haloaryl N-tosylhydrazones has been developed. The thermo-induced isomerization of N-tosylhydrazones is discussed. A series of valuable indazole derivatives are prepared in good yields, and the method has been successfully applied to the synthesis of the bioactive compounds, lonidamine, AF-2785, axitinib, YC-1 and YD-3.
