covalent binding

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.

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.

MS8511, a selective covalent irreversible inhibitor of G9a GLP, targets a cysteine residue at the substrate binding site, displaying IC50 values of 100 nM (G9a) and 140 nM (GLP), alongside Kd values of 44 nM (G9a) and 46 nM (GLP). This compound effectively reduces cellular H3K9me2 levels and boosts antiproliferation activity, making it applicable in cancer research involving brain, breast, ovarian, lung, bladder, melanoma, and colorectal cancers, as well as studies on Alzheimer's disease (AD), sickle cell disease, and Prader−Willi syndrome (PWS) [1].

MS8511 HCl is a selective and potent covalent inhibitor of G9a GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer activity and antiproliferative activity and reduces intracellular H3K9me2 levels.MS8511 can be used to study a wide range of cancers including brain, breast, and ovarian cancers .

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 effects on pHER2 and EGF.

USP7-797 is a selective non-covalent active site USP7 inhibitor, inhibiting USP7 and ubiquitin binding, with anti-tumor, oral and high efficiency (IC50=0.44 nmol), it is effective on both wild-type and mutant p53 tumor cells, and can significantly inhibit the growth of tumor cells and induce apoptosis.

Zebularine (4-Deoxyuridine) is a DNA methylation inhibitor. Acts as a transition state analog inhibitor of cytidine deaminase by binding to the active size as covalent hydrates. It also inhibits cytidine deaminase (Ki: 2 μM, in a cell-free assay).

THZ1 (CDK7 inhibitor) is a selective covalent inhibitor of CDK7, exhibiting binding affinity to the cysteine residue located at the outer end of the classical kinase domain, thus conferring high selectivity for CDK7, with an IC50 of 3.2 nM.

AMG410 is a non-covalent, dual-modality KRAS inhibitor effective against both GDP (OFF) and GTP (ON) binding, with Kd (GDP) of 1 nM and Kd (GTP) of 22 nM, capable of blocking KRAS independently of the cell cycle. AMG410 does not affect HRAS and NRAS2, and exhibits high potency against KRAS G12D, G12V, G12C, G13D, and other mutants, with an IC₅₀ of 1–4 nM. It induces tumour regression and reduces phosphorylated ERK levels in KRAS-mutant cancer models.

RMC-6291 is an orally active, covalent inhibitor of KRAS G12C (ON) that forms a tri-complex within tumor cells between KRAS G12C (ON) and cyclophilin A (CypA), thereby preventing KRAS G12C (ON) from signaling via steric blockade of RAS effector binding and eliciting deep and durable suppression of RAS pathway activity in KRAS G12C tumor models [1].

UbcH5c-IN-1 is a selective small-molecule Ubiquitin-conjugating enzyme UbcH5c inhibitor (Kd: 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85).

Pimonidazole hydrochloride accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after the reduction of its nitro group. It can be used for qualitative and quantitative assessment of tumor hypoxia. Pimonidazole hydrochloride is a novel hypoxia marker for the complementary study of tumor hypoxia and cell proliferation in tumors.

Pimonidazole accumulates in hypoxic cells via covalent binding with macromolecules or by forming reductive metabolites after the reduction of its nitro group. It can be used for qualitative and quantitative assessment of tumor hypoxia. Pimonidazole is a n

Zipalertinib (TAS6417, CLN-081) is a novel, highly potent, orally active covalent EGFR tyrosine kinase inhibitor that uniquely binds to the ATP binding site of the EGFR hinge region with an IC50 value of 1.1-8.0 nM.

TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling. TX1-85-1 is an irreversible Her3 inhibitor (IC50: 23 nM). TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in th

Triazophos is a non-systemic pesticide that acts as an acetylcholinesterase (AChE) inhibitor, forming a covalent and irreversible bond with the acetylcholine binding site. This action blocks the hydrolysis of acetylcholine, leading to increased excitability. It is effective against a wide range of soil insects and mites, including aphids, thrips, midges, beetles, lepidopteran larvae, mole crickets, and red spiders. Triazophos is suitable for use on various crops such as ornamental plants, cotton, rice, corn, soybeans, oil palm, olives, and coffee.

FAPI-mFS, an irreversible fibroblast activation protein (FAP) inhibitor, enhances uptake and retention in cancer cells through its covalent binding properties with FAP. When labeled with radioactive 68Ga or 177Lu, FAPI-mFS can be utilized for cancer imaging and therapy.

MS8511 (hydrochloride) is a specific covalent and irreversible inhibitor of G9a GLP, targeting the cysteine residue at the substrate binding site. It has an IC50 of 100 nM for G9a and 140 nM for GLP, with Kd values of 44 nM for G9a and 46 nM for GLP. This compound reduces intracellular H3K9me2 levels and enhances antiproliferative activity, making it useful for studying various cancers, including brain, breast, ovarian, lung, bladder cancers, melanoma, and colorectal cancer, as well as other diseases like Alzheimer's disease (AD), sickle cell disease, and Prader-Willi syndrome (PWS).

DPP8/9-IN-1 (Compound 16) is a selective covalent inhibitor of dipeptidyl peptidase 8 and 9 (DPP8/9), with IC50 values of 14 nM and 298 nM, respectively. It irreversibly binds to the active site serine (such as S730 in DPP9) through a phosphate ester warhead, blocking substrate binding and inhibiting DPP8/9-mediated protein processing. DPP8/9-IN-1 holds potential for research in cancer and inflammatory diseases.

VVD-699 is a covalent inhibitor of RAS-PI3K. It forms a covalent bond with cysteine at position 242 within the RAS-binding domain of PI3Kp110α, thereby obstructing the ability of RAS to activate PI3K. VVD-699 is capable of inhibiting the growth of tumors with RAS mutations and HER2 overexpression. It is applicable in research related to RAS mutation-associated cancers, such as those involving H358 lung cancer cells, A549 cells, and FaDu cells.

AX-53802 is a ferroptosis (ferroptosis) inducer targeting GPX4, with an IC50 of 0.34 µM. It forms a covalent bond with GPX4, initiating membrane translocation upon binding. In combination with FAK/Src inhibitors, AX-53802 enhances cell death. This compound is applicable in cancer research.

Chlorotris (triphenylphosphine) copper (CuCl(TPP)₃) is a metal complex that targets DNA. Through non-covalent interactions of its copper (I) center, such as groove-binding, it affects DNA function and exhibits inhibitory activity against bacteria, fungi, and tumor cells. Chlorotris (triphenylphosphine) copper holds potential for research as an antimicrobial, antitumor, and antioxidant agent.

TLCD1-IN-1 (compound MB-4A) is a covalent inhibitor of TLCD1. It demonstrates stereoselective binding and activity inhibition of TLCD1 in HepG2 cells.

Folitixorin (ANX-510) is an active folate derivative and coenzyme associated with thymidine synthesis, with potential antitumour activity.