covalent — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T11709	JAK3 covalent inhibitor-1		JAK
	JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and demonstrating a 246-fold selectivity compared to other JAKs.		JAK
T41277	PACMA 31		Others
	PACMA 31 is an irreversible and covalent inhibitor of protein disulfide isomerase (PDI) with an IC50 of 10 μM. PACMA 31 significantly suppresses ovarian tumor growth and exhibits tumor targeting ability.		Others
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
T3583	Macozinone	PBTZ169	Antibacterial , DprE1
	Macozinone (PBTZ169) inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043.		Antibacterial , DprE1
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
T8371	ML188		Virus Protease , SARS-CoV
	ML188 is a selective noncovalent SARS-CoV 3CLpro inhibitor(IC50 : 1.5 μM), with moderate MW and good enzyme and antiviral inhibitory activity.		Virus Protease , SARS-CoV
T9061	EN4	EN4 MYC inhibitor	c-Myc
	EN4 (EN4 MYC inhibitor) MYC inhibitor is a covalent ligand that targets cysteine 171 (C171) of MYC. It is selective for c-MYC over N-MYC and L-MYC, and inhibits MYC transcriptional activity, downregulates MYC targets, an...		c-Myc
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
T22461	YKL-5-124		CDK
	YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7/Mat1/CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12/13...		CDK
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
T8926	Salcaprozate sodium	SNAC	Others
	Salcaprozate sodium (SNAC), an oral absorption promoter, serves as a potent delivery agent for oral heparin and insulin by enhancing passive transcellular permeation through small intestinal epithelia. This is achieved t...		Others
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
T10460	Batabulin	T138067	Apoptosis , Microtubule Associated
	Batabulin (T138067) is an antitumor compound, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to ce...		Apoptosis , Microtubule Associated
T8421	TED-347		YAP
	TED-347 is an irreversible and covalent inhibitor of TEAD4-Yap1 protein-protein interaction(EC50 of 5.9 μM), and inhibits glioblastoma cell viability.		YAP
T10898	Samuraciclib hydrochloride	ICEC0942 hydrochloride,CT7001 hydrochloride	Apoptosis , CDK
	Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold h...		Apoptosis , CDK
T2256	CNX-1351		PI3K
	CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor.		PI3K
T8307	Hydroxy-α-sanshool	Hydroxy-α-sanshool	Endogenous Metabolite , TRP/TRPV Channel
	Hydroxy-α-sanshool is an alkyl amide isolated from the pepper. It acts as a TRPA1 covalent and TRPV1 non-covalent agonist (EC50s: 69 and 1.1 μM).		Endogenous Metabolite , TRP/TRPV Channel
T79659	SARS-CoV-2 3CLpro-IN-16		SARS-CoV
	SARS-CoV-2 3CLpro-IN-16 is a covalent SARS-CoV-2 3CLpro inhibitor that inhibits 3CLpro activity and achieves its inhibitory effect by forming a covalent bond with Cys145.		SARS-CoV
T7609	ARS-1620		Ras
	ARS-1620 is a covalent inhibitor of K-RASG12C.		Ras
T60096	EN106	ZINC3888023	Others
	EN106, a potent FEM1B inhibitor and a cysteine-reactive covalent ligand, effectively disrupts the recognition of FEM1B's crucial reductive stress substrate, FNIP1.		Others