k 12

LL-K12-18 is a dual-site molecular gel that enhances protein-protein interactions (PPIs) between CDK12-DDB1 complexes thereby promoting the degradation of Cyclin K. It potently inhibits tumor cell gene transcription and anti-proliferation.

LL-K12-18 is a two-site molecular glue that enhances interaction between CDK12 and DDB1, stabilizing the complex and promoting selective degradation of cyclin K with an EC50 of 0.37 nM. It exhibits potent transcriptional repression and antiproliferative effects in tumor models, making it a valuable chemical tool for investigating transcriptional regulation and targeted protein degradation in cancer research.

CDK12-Cyclin K ligand-1 is a ligand for PROTAC degraders, designed to bind with E3 ligase. It is utilized in synthesizing PROTAC degraders, such as [PP-C8].

CDK12-Cyclin K Ligand-Linker Conjugates 1 is a Target Protein Ligand-Linker Conjugate that includes a CDK12-Cyclin K ligand and a PROTAC linker, which can recruit E3 ligase. CDK12-Cyclin K Ligand-Linker Conjugates 1 is applicable for the synthesis of PROTACPP-C8.

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).

K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of the oncogenic K-Ras(G12C) protein.

K-Ras G12C-IN-1 is a novel, irreversible inhibitor of mutant K-Ras G12C.

K-Ras G12C-IN-2 is a covalent KRAS G12C inhibitor.

Heterocyclic compounds as covalent inhibitors of G12C mutant K-Ras protein useful for treating cancers.K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.

K-Ras G12C-IN-4, is a potent Covalent Inhibitor of KRASG12C..

K-Ras(G12C) inhibitor 6 is an irreversible, allosteric inhibitor of the K-Ras(G12C) mutant, achieving 100% protein modification at 10 μM after 24 hours in vitro.

PI3K/mTOR Inhibitor-12, a potent and selective orally active inhibitor, exhibits IC50 values of 0.06 nM for PI3Kα and 3.12 nM for mTOR, indicating significant antitumor activity with reduced liver toxicity [1].

PI3Kδ-IN-12 (compound 13), a PI3Kδ inhibitor with a pIC50 of 5.8, exhibits differential binding affinities with pKi values of 8.0 for PI3Kδ, 6.5 for PI3Kγ, 6.4 for PI3Kβ, and 6.7 for PI3Kα. This compound is used in researching chronic respiratory conditions, including asthma and chronic obstructive pulmonary disease (COPD) [1].

PI3Kα-IN-12 (compound 13), a potent and selective PI3Kα inhibitor (IC50: 1.2 nM), effectively suppresses HCT-116 and U87-MG cell proliferation with IC50 values of 0.83 and 1.25 μM, respectively. Intraperitoneal administration of PI3Kα-IN-12 (40 mg/kg) induces tumor regression in a mouse xenograft model bearing U87-MG cells [1].

SDK-12B-5 is an innovative antitumor compound. Administered orally every other day, SDK-12B-5 maximizes chemotherapy effects while minimizing cumulative toxicity.

EUK 124 is an inhibitor of superoxide-mediated reduction of an electron acceptor.

BK 129 is a local anesthetic with relaxant properties. BK 129 inhibits Ca2+ entry into the smooth muscle cell and Ca2+ release from sarcoplasmic reticulum.

K 12425 is a bioactive chemical.

Dexamethasone is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory, immunosuppressive, and apoptosis-inducing activities. It inhibits the production of inflammatory miRNA-155 exosomes in macrophages, significantly reduces inflammatory cytokine expression in neutrophils and monocytes, suppresses LPS-induced macrophage inflammation, and induces autophagy. It is commonly used to induce animal models of depression, muscle atrophy, and hypertension, and holds potential in COVID-19 research.

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1/26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

ERK1/2 inhibitor 1 is a potent, orally bioavailable compound that exhibits 60% inhibition at 1 nM and has an IC50 of 3.0 nM against ERK1 and ERK2, respectively.

Cdk1/2 Inhibitor III is a selective inhibitor of Cdk1/2 with an IC50 value of 2.1 μM against CDK1/cyclin B.

CDK12-IN-3 is a selective and potent CDK12 inhibitor with anti-tumor activity, which can be used to study malignant tumors.