conformation — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
TP1263	Fz7-21	(Ac)-LPSDDLEFWCHVMY-NH2	Wnt/beta-catenin
	Fz7-21 ((Ac)-LPSDDLEFWCHVMY-NH2) is a peptide antagonist of FZD7 . It antagonises WNT3A-induced Wnt-β-catenin signalling in HEK293 expressing FZD7. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with e...		Wnt/beta-catenin
T19802	B-Raf IN 11		Raf
	B-Raf IN 11 is a novel selective inhibitor. The DFG-in conformation of the B-Raf kinase V600E mutant is superior to the DFG-out conformation in colorectal cancer.		Raf
T28267L	(+)-ORM-10921		Others
	(+)-ORM-10921 is a conformation of ORM-10921 and can be used in chemical synthesis studies.		Others
T37807	JTV 519 fumarate
	Ryanodine receptor (RyR) inhibitor; stabilizes RyR2 in a closed conformation. Exhibits antiarrhythmic and cardioprotective properties in vivo. Hunt et al (2007) K201 (JTV519) suppresses spontaneous Ca2+ release and [3H]r...
T34760	SYR127063	SYR-127063,BDBM 92454,SYR 127063,BDBM-92454,BDBM92454	EGFR , HER
	SYR127063 (BDBM-92454) (BDBM92454) is a potent and selective HER2 inhibitor, binds to HER2 in a reactive conformation.		EGFR , HER
T5938	4-Phenoxybenzylamine		HCV Protease
	4-Phenoxybenzylamine inhibits the function of the NS3 protein by stabilizing an inactive conformation with an IC50 of about 500 μM against HCV NS3/4a .		HCV Protease
T8864	Thymidylate Kinase Inhibitor, YMU1		Others
	YMU1 is a human thymidylate kinase (hTMPK) inhibitor. YMU1 stabilizes the conformation of ligand-induced degradation (LID) region of hTMPK and blocks the catalytic site or ATP-binding site.		Others
T25210	CBHcy		Transferase
	CBHcy is a dual-substrate analogue, a specific BHMT inhibitor that causes betaine-homocysteine S-methyltransferase (BHMT) to adopt the same conformation as the ternary complex, potentially inducing the development of cys...		Transferase
T21648	CP-31398 dihydrochloride	CP 31398 dihydrochloride	p53
	CP-31398 dihydrochloride is a p53 stabilizer which stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53.		p53
T22980	MIRA-1	p53 Activator VIII,1-[(1-Oxopropoxy)methyl]-1H-pyrrole-2,5-dione,(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)methyl propionate,NSC 19630,WRN Helicase Inhibitor	DNA/RNA Synthesis , p53
	MIRA-1 (WRN Helicase Inhibitor) is a restorer of wild-type p53 conformation/cellular function and selectively inhibits Werner syndrome WRN helicase activity with an IC50 of 20 µM.		DNA/RNA Synthesis , p53
T4414	Eprenetapopt	APR-246,PRIMA-1Met	Apoptosis , Others , Ferroptosis , p53 , Autophagy
	Eprenetapopt (PRIMA-1Met) restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1MET also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of c...		Apoptosis , Others , Ferroptosis , p53 , Autophagy
T9095	Necrostatin-34	2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4	RIP kinase
	Necrostatin-34 (2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4) is a RIPK1 kinase inhibitor, stabilizing RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain.		RIP kinase
T8799	(E/Z)-IT-603	IT603	Others , NF-κB
	(E/Z)-IT-603 is a cell-permeable c-Rel inhibitor (IC50: 3μM). IT-603 directly and reversibly binds to c-Rel to change its conformation and blocks its DNA binding and transcriptional activity.		Others , NF-κB
T8684	Sotorasib	AMG-510	Ras
	Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib ...		Ras
T8655	SR-717		STING
	SR-717 is a cGAMP analog, a non-nucleoside STING agonist that induces a "closed" activation conformation of STING. SR-717 has antitumor activity and promotes activation of immune cells and cross-presentation of antigens.		STING
T8369	Adagrasib	MRTX849	Ras
	Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib ...		Ras
TP2068L	Cyclotraxin B acetate(1203586-72-4 free base)		Trk receptor
	Cyclotraxin B acetate is an antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold...		Trk receptor
T61822	M1002		HIF
	M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist that enhances the affinity of HIF-2alpha and ARNT for transcriptional activation.M1002 alters the Tyr2 conformation of the HIF-281alpha PAS-B structural domain and ac...		HIF
T9172	Simufilam dihydrochloride	PTI-125 dihydrochloride	Others
	Simufilam dihydrochloride (PTI-125 dihydrochloride) is a low toxicity, orally active filamin A (FLNA) activator, which can be used for the research of Alzheimer's disease. Simufilam dihydrochloride preferentially binds a...		Others
T24076	FzM1	FzM 1,FzM-1	Wnt/beta-catenin
	FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2) by binding to an allosteric site on intracellular loop 3 (ICL...		Wnt/beta-catenin