cyclin

O6-Benzylguanine is a guanine analog with antineoplastic activity,and is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM, effectively suppressing the proliferation of human gastric cancer cells by downregulating the PAK4/c-Src/EGFR/cyclin D1 pathway and inducing apoptosis.

Purvalanol B (NG 95) is a CDK inhibitor that targets Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p35, and Cdk2/cyclin B, with IC50 values of 6, 9, 6, and 6 nM, respectively.

SW106065 is a novel pharmacologic inducer of apoptosis in MPNST (malignant peripheral nerve sheath tumors).SW106065 is an apoptosis inducer in malignant peripheral nerve sheath tumors (MPNST). It inhibits ATP consumption of sMPNST and other models of MPNST with an EC50 of 1 μM. SW106065 can be used for MPNST 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.

Cyclin A/B RxL-IN-1 is an inhibitor targeting the interaction between Cyclin A/B RxL and the hydrophobic patch (HP). It exhibits an IC50 of 0.12 μM for inhibiting Cyclin A. In xenograft models derived from murine cell lines (CDX), Cyclin A/B RxL-IN-1 demonstrates antitumor efficacy. CDK-IN-19 is applicable for research on E2F-driven cancers, including small cell lung cancer (SCLC).

Cyclin A/B RxL-IN-2 is a macrocyclic peptide Cyclin A/B inhibitor with oral bioavailability. It exhibits an IC50 of 0.05 μM and a Kd of 2.7 nM for Cyclin A, and an IC50 of less than 0.02 μM and a Kd of 1.0 nM for Cyclin B. This compound competitively binds to the hydrophobic pocket (HP) of Cyclin A/B, blocking their interaction with substrate RxL motifs, inducing replication stress, DNA damage, mitosis, and apoptosis in E2F overexpressing cells. In NCI-H69 and NCI-H446 small cell lung cancer xenograft models, Cyclin A/B RxL-IN-2 demonstrates tumor growth inhibition and regression, making it useful for related small cell lung cancer research.

Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL), a CDK2 inhibitor, exhibits dose-dependent cytotoxic effects on U2OS osteosarcoma cells [1].

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC MDA-MB-231 cells with an IC50 of 0.044 μM and inducing apoptosis. This compound diminishes CDK9 transcriptional activity and downregulates phosphorylation of RNA Pol II CTD ser2. In vivo, CDK9-Cyclin T1 PPI-IN-1 effectively impedes tumor growth in a TNBC 4T1 mouse model [1].

Cyclin K degrader 1 is a Cyclin K degrader.Cyclin K degrader 1 is a degrader converted from AT-7519.Cyclin K degrader 1 has weak degrading activity against Cyclin K but does not result in a sustained decrease in degradation affinity.Cyclin K degrader 1 is a degrader converted from AT-7519.

Cyclin-dependent kinase 2 also known as cell division protein kinase 2. The protein encoded by this gene is a member of the cyclin-dependent kinase family of Ser/Thr protein kinases. This protein kinase is highly similar to the gene products of S. cerevis

Nimbolide, a triterpenoid derived from neem leaves and flowers, is a natural product and a CDK4/CDK6/NF-κB inhibitor that inhibits multiple signaling pathways including Wnt and PI3K-Akt, possesses antitumor activity, and can induce tumor cell apoptosis.

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycetes, functioning as an XBP1 inhibitor and inhibiting IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM), and induces apoptosis.

Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.

Dinaciclib (SCH 727965) is a selective CDK inhibitor targeting CDK1, CDK2, CDK5, and CDK9 (IC50 = 3/1/1/4 nM). It exhibits potential antitumor activity by inhibiting the incorporation of thoracic glycan (dThd) DNA.

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

Flavopiridol (Alvocidib) (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.

5-Iodo-indirubin-3'-monoxime is a potent inhibitor of GSK-3β, CDK5/P25, and CDK1/cyclin B, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20, and 25 nM).

Abemaciclib metabolite M20 (CDK4/6-IN-4) is an active metabolite of Abemaciclib. Abemaciclib metabolite M20 is a selective CDK4/6 inhibitor and can be used for researches on the treatment of cancer.

SEL120-34A HCl is a selective, orally available and ATP-competitive inhibitor of CDK8(CDK8/CycC and CDK19/CycC with IC50s of 4.4 nM and 10.4 nM , respectively), with antitumor activity.

CDK9-IN-7 is a highly selective and orally active CDK9/cyclin T inhibitor (IC50: 11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD: 148 nM; CDK6/cyclinD: 145 nM).

CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor [IC50: 2.3 nM].