LY364947(LY-364947)|cas 396129-53-6|DC Chemicals

Cas No.:	396129-53-6
Chemical Name:	4-(3-Pyridin-2-YL-1H-pyrazol-4-YL)quinoline
Synonyms:	4-(3-(Pyridin-2-yl)-1H-pyrazol-4-yl)quinoline;LY-364947;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline;[3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole;LY364947;4-(3-Pyridin-2-yl-1H-pyrazol-4-yl)quinoline;LY364947 (LY-364947, HTS 466284);4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline;HTS466284;Transforming Growth Factor-β Type I Receptor Kinase Inhibitor;E 616451;TGF-beta RI Kinase Inhibitor;HTS 466284;TbetaR-I Inhibitor;LY 364947;4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]quinoline;4-[5-(pyridin-2-yl)-1H-pyrazol-4-yl]quinoline;Quinoline, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-;Transforming Growth Factor-beta Type I Receptor Kinase Inhibitor;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline;4-(3-pyridin-2-yl)(1h)-pyra
SMILES:	N1([H])C(C2=C([H])C([H])=C([H])C([H])=N2)=C(C([H])=N1)C1=C([H])C([H])=NC2=C([H])C([H])=C([H])C([H])=C12
Formula:	C₁₇N₄H₁₂
M.Wt:	272.304
Sotrage:	2 years -20°C powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	LY-364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
In Vivo:	LY-364947 (1 mg/kg, i.p.) accelerates lymphangiogenesis, as evidence by significantly increasing the LYVE-1-positive areas in a mouse model of chronic peritonitis. LY-364947 (1 mg/kg, i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells[2]. LY-364947 (25 mg/kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice[3].
In Vitro:	LY-364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I Kinase with Ki of 28 nM. LY-364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY-364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY-364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY-364947 (2 μM) prevents TGF-β-induced epithelial−mesenchymal transition in NMuMg cells[1]. LY-364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours[2]. LY-364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY-364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells[3].

Cat. No.	Product name	Field of application
DC82301	IC-8	IC8 is an ionizable cationic lipid. It has been used in combination with other lipids for the formation of lipid nanoparticles (LNPs). Immunization with severe acute respiratory coronavirus 2 (SARS-CoV-2) spike glycoprotein mRNA in IC8- and manganese-containing LNPs induces IgG responses to SARS-CoV-2 Delta and Omicron variants in mice.1 Administration of mRNA encoding B7-H3 X CD3 bispecific T cell engaging (BiTE) antibodies in IC8-containing LNPs reduces tumor growth in MV4-11 and A375 mouse xenograft models.
DC75721	CL2A-SN38 (Govitecan)	CL2A-SN38 is a SN38 derivative with a peptide-linker which can easily react with antibody to form an antibody-drug conjugate (ADC). CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .
DC47877	tri-GalNAc-COOH (acetylation)	tri-GalNAc-COOH acetylation is the acetylated and modified form of tri-GalNAc-COOH. tri-GalNAc-COOH acetylation can be used for the synthesis of LYTAC.
DC46965	Tri-GalNAc-COOH	tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.
DC46471	RP101988	RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely.
DC37901	PD-173212	PD-173212 is a small molecule N-type calcium channel blocker.
DC37333	N,N-Diethyl-p-toluamide	N,N-Diethyl-p-toluamide is a mosquito repellent.
DC37321	AI3-15902	AI3-15902 is a biochemical.
DC37283	Methyl phenylcarbamate	Methyl phenylcarbamate is a biochemical.
DC37252	Ampyrone	Ampyrone is a metabolite of AMINOPYRINE with analgesic and anti-inflammatory properties. It is used as a reagent for biochemical reactions producing peroxides or phenols. Ampyrone stimulates LIVER MICROSOMES and is also used to measure extracellular water.