selective,covalent

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

RMC-9805 is a novel, mutant-selective, covalent and oral KRASG12D (ON) inhibitor. A stable and high affinity triple complex is formed between RMC-9805, KRASG12D, and cyclophilin A, which inhibits signal transduction downstream of KRASG12D (ON) by disrupting its interaction with downstream effectors. RMC-9805 can induce cell apoptosis and promote tumor regression in preclinical KRASG12D tumor models. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.

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.

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.

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.

GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.

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.

MKK7-COV-9 is a selective and potent covalent inhibitor of MKK7 with inhibitory effects on MKK7-induced protein-protein interactions.MKK7-COV-9 interrupts the activation of primary B-cells in response to LPS.MKK7-COV-9 shows low cytotoxicity at high concentrations.

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.

CNX-1351 is a potent, isoform-selective, and targeted covalent inhibitor of PI3Kα.

EGFR-IN-2 is a non-covalent, orally available and mutation-selective EGFR inhibitor for the treatment of non-small cell lung cancer (NSCLC), with high selectivity for resistant single and double mutant T790M with IC50 = 27 nm to 33 nM, and low inhibitory activity for wild-type H292 (IC50 = 218 nM).

Faldaprevir is an orally effective, selective, non-covalent HCV NS3 4A protease inhibitor with high inhibitory activity against HCV 1a and 1b genotypes (Ki=2.6 nM &2.0 nM).Faldaprevir inhibits viral replication by blocking the breakdown of viral precursor proteins, and is well tolerated with good antiviral activity against hepatitis C virus.

PBRM (17β-HSD1-IN-2) is a selective covalent inhibitor of 17β-HSD1, used in breast cancer and endometriosis research.

FT671 is a non-covalent and selective inhibitor of USP7 (IC50: 52 nM) It also binds to the USP7 catalytic domain (Kd: 65 nM).

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.

ML-210 (CID 49766530) is a glutathione peroxidase 4 (GPX4) inhibitor (EC50=30 nM) that is covalent and selective. ML-210 has antitumor activity and induces ferroptosis.

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.

GSK4418959 (IDE275) is an orally active, non-covalent, reversible, and selective WRN helicase inhibitor. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used to study MSI-H related research.

bio-THZ1 is a biotinylated version of THZ1, a selective and irreversibly covalent CDK7 inhibitor (IC50: 3.2 nM).

Nazartinib mesylate is a novel, covalent mutant-selective inhibitor of EGFR (Ki and Kinact: 31 nM and 0.222 min on EGFR(L858R 790M) mutant).