selective,covalent — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T16143	MRTX-1257		Ras
	MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C. It has an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. MRTX1257 demonstrated 31% bioavailability in the mouse, with fre...		Ras
T7414	ARS-853		Apoptosis , Raf , Ras
	ARS-853 is an inhibitor of K-RASG12C(IC50 : 2.5 μM), a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells		Apoptosis , Raf , Ras
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
T2256	CNX-1351		PI3K
	CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor.		PI3K
T13044	Mevociclib	SY-1365	CDK
	Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7. SY-1365 possesses therapeutic potential in both hematological and solid tumors.		CDK
T67933	BAY-4931		PPAR
	BAY-4931 is a powerful, covalent, and selective inverse-agonist of PPARγ, exhibiting an IC50 value of 0.17 nM.		PPAR
T16515	PF 750	PF-750,UNII-7756CPP14K,ZINC27647189	FAAH
	PF 750 (ZINC27647189) is a selective and covalent inhibitor of FAAH. PF 750 shows IC50s varying from 16.2 to 595 nM in different incubation times.		FAAH
T3664	THZ1	CDK7 inhibitor,THZ1 2HCl	CDK
	THZ1 (CDK7 inhibitor) is a novel selective and potent covalent CDK7 inhibitor.		CDK
T15351	FT827		DUB
	FT827 is a covalent inhibitor of selective ubiquitin-specific protease 7 (USP7) (Ki=4.2 µM, Kd=7.8 µM) targeting the catalytic center of the autoinhibitory apolipoprotein form of USP7 for cancer research.		DUB
T9303	MRTX1133		Ras
	MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.		Ras
T12542	Rilzabrutinib	PRN1008	EGFR , Others , HER , BTK
	Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK)(IC50 of 1.3 nM).		EGFR , Others , HER , BTK
T5825	Iadademstat dihydrochloride	ORY-1001(trans)	Histone Demethylase
	Iadademstat dihydrochloride (ORY-1001(trans)) , a Potent and Selective Covalent KDM1A/LSD1 Inhibitor, for the Treatment of Acute Leukemia.		Histone Demethylase
T22306	DGY-06-116		FGFR , Src
	DGY-06-116 is an selective and irreversible covalent inhibitor of Src and FGFR1 with IC50 value of 3nM and 8340 nM, respectively.		FGFR , Src
T5407	Branebrutinib	BMS986195	BTK
	Branebrutinib (BMS986195) is a potent, covalent inhibitor of Bruton's tyrosine kinase (BTK), >5,000-fold selective over all kinases outside of the Tec family (IC50 <1 nM for BTK).		BTK
T11724	JNJ-42226314		Lipase
	JNJ-42226314 is a highly selective non-covalent monoacylglycerol lipase (MAGL) inhibitor with anti-injury effects.JNJ-42226314 shows efficacy via endogenous cannabinoid-2-acryloylglycerol (2-AG) in models of neuropathic ...		Lipase
T9203	JH-X-119-01		IRAK
	JH-X-119-01 is a highly potent and selective covalent inhibitor of IRAK-1.		IRAK
T8375	ML-210	CID 49766530	Ferroptosis , GPX , Glutathione Peroxidase , Ras
	ML-210 (CID 49766530) is a selective RAS and covalent glutathione peroxidase 4 (GPX4) inhibitor(GPX4, EC50 : 30 nM), with anti-cancer activity		Ferroptosis , GPX , Glutathione Peroxidase , Ras
T9240	Sulfopin	Acetamide, 2-chloro-N-(2,2-dimethylpropyl)-N-(tetrahydro-1,1-dioxido-3-thienyl)-	Others
	Sulfopin is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17nM. Sulfopin blocks Myc-driven tumors in vivo.		Others
T69534	Zongertinib	BI 764532,BI 1810631	Tyrosine Kinases , HER
	Zongertinib is a human HER2-selective tyrosine kinase inhibitor, a novel TK that is highly selective for covalent binding to the HER2 tyrosine kinase domain (TKD).Zongertinib exhibits antitumor activity with inhibitory e...		Tyrosine Kinases , HER
T39738	ASP2453		Ras
	ASP2453 is a potent, selective and covalent inhibitor of KRAS G12C. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.		Ras