covalent inhibitor

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.

JAK3covalent inhibitor-2 (compound J1b) is a selective JAK3 inhibitor with oral efficacy, boasting an IC50 value of 7.2 nM. It is characterized by low toxicity, anti-inflammatory properties, and excellent bioavailability.

GRL0617 is a selective and competitive noncovalent inhibitor of SARS-CoVPLpro and deubiquitinase (IC50: 0.6 μM, Ki: 0.49 μM).

Daraxonrasib (RMC-6236) is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.

RMC-9805 (Zoldonrasib) is a mutant-selective covalent KRAS G12D inhibitor with oral activity and significant antitumor activity, inducing tumor cell apoptosis in preclinical models of various KRAS-mutant cancers.

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.

Gut restricted-7 (GR-7) is a potent, covalent, orally administered, gut-selective bile salt hydrolase (BSH) inhibitor with tissue specificity that localizes to the gut. Gut restricted-7 reduces BSH activity in gut bacteria and decreases levels of unconjugated bile acids in mouse feces, making it suitable for research into metabolism, inflammation, and intestinal diseases.

Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue.

Remibrutinib (Rhapsido) belongs to small molecule inhibitors and is a highly selective, covalent Bruton's tyrosine kinase (BTK) inhibitor (IC50 = 1 nM) with oral activity and cell permeability. The IC50 for inhibiting BTK activity in blood is 0.23 μM. This compound can be used in research on chronic urticaria.

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

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 exhibits inhibitory activity against KRAS G12C mutant tumors.

MY-1B is a covalent inhibitor and an inhibitor of RNA methyltransferase NSUN2 (IC50 = 1.3 μM), featuring stereoselectivity, covalent binding to C271 of NSUN2, and the ability to target PSME1, disrupt proteasome regulatory complexes, and downregulate presentation of specific MHC-I subtypes.

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 exhibits inhibitory activity against KRAS G12C mutant tumors.

ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor that induces ferroptosis. ML162 has antitumor activity and selectively inhibits cell lines expressing mutant RAS oncogenes.

GSK3685032 is a time-independent, non-covalent, selective, and reversible DNMT1 inhibitor with an IC₅₀ of 0.036 μM. GSK3685032 induces loss of DNA methylation, transcriptional activation, and inhibition of cancer cell growth, and can be used in cancer therapy research.

6RK73 is a covalent, irreversible, and specific UCHL1 inhibitor (IC50: 0.23 µM) with almost no inhibition of UCHL3 (IC50: 236 µM).

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.

BSH-IN-1 is a potent, covalent inhibitor of gut bacterial recombinant bile salt hydrolases (BSHs; IC50s: 108 nM for B. longum BSH and 427 nM for B. theta BSH).

GSK-3484862 is a non-covalent Dnmt1 inhibitor that induces DNA hypomethylation, offering potential therapeutic benefits against cancer.

RMM-46 is a reversible covalent inhibitor with high ligand efficiency and selectivity for MSK/RSK family kinases.

FIIN-4 is a covalent inhibitor of FGFR and can be used in studies about metastatic breast cancer.

JAK3i is a selective covalent inhibitor of JAK3 kinase. JAK3i reveals two distinct temporal waves of STAT5 phosphorylation and more potently targets the second wave, which is required for cell cycle progression and T cell proliferation.

SY-5609 (CDK7-IN-3) is a selective non-covalent CDK7 inhibitor (Kd value is 0.07 nM), with weak inhibitory activity against CDK2, CDK9 and CDK12 with IC50 values ​​of 5.5, 1.9 and 1.7 μM, respectively, and has anti-tumor activity and inhibits cell apoptosis.

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.