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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. | |||
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. | |||
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... | |||
T3583 | Macozinone | PBTZ169 | Antibacterial , DprE1 |
Macozinone (PBTZ169) inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043. | |||
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 | |||
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. | |||
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... | |||
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 ... | |||
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... | |||
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 | |||
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... | |||
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 ... | |||
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... | |||
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. | |||
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... | |||
T2256 | CNX-1351 | PI3K | |
CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor. | |||
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. | |||
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). | |||
T7609 | ARS-1620 | Ras | |
ARS-1620 is a covalent inhibitor of K-RASG12C. | |||
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. |