CDK Inhibitor

M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC₅₀ value of 0.09  μM. M2N12 also has promising activity against Cdc25A and Cdc25B with IC₅₀ values of  0.53  μM and 1.39 μM, respectively. M2N12 has anti-tumor activity and can be used for cancer research.

DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC₅₀ of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK.

Cdc7-IN-1 (Compound 13) is a highly potent, selective and ATP competitive inhibitor of Cdc7 kinase, with an IC₅₀ value of 0.6 nM at 1 mM ATP and with slow off-rate characteristics. Cdc7-IN-1 potently inhibits Cdc7 activity in cancer cells, and effectively induces cell death.

LH2-051, a lysosome-enhancing compound (LYEC), is a brain-penetrant dopamine transporter (DAT) inhibitor (K_i: 0.95 μM). LH2-051 inhibits DAT-mediated dopamine uptake with an IC₅₀ of 3.0 μM. LH2-051 promotes nuclear translocation of TFEB and lysosome biogenesis. LH2-051 improves the memory of amyloid precursor protein (APP)/Presenilin 1 (PS1) mice. LH2-051 can be used for the study of Alzheimer’s disease.

Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor.

CDK8-IN-4 is an inhibitor of CDK8 extracted from patent WO2014090692A1, compound example 16, with an IC₅₀ of 0.2 nM.

CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC₅₀s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth.

CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compound, is a CDK inhibitor with anticancer activities.

(S)-PHA533533 is a CDK2 and CDK5 inhibitor with blood-brain barrier permeability, with IC₅₀ values of 37 nM and 55 nM, respectively. (S)-PHA533533 effectively restores UBE3A expression by downregulating UBE3A-ATS and relieving the epigenetic silencing of paternal UBE3A in mature neurons. (S)-PHA533533 can be used for the research of Angelman syndrome.

Crozbaciclib (CDK4/6/1 Inhibitor) is a CDK4/6 inhibitor with IC₅₀s of 3 and 1 nM, respectively.

FMF-04-159-R is a cyclin-dependent kinase CDK14 and CDK16 inhibitor with IC₅₀ values of 5.9 and 139.1 nM.

Eciruciclib is an antineoplastic and potent cyclin dependent kinase (CDK) inhibitor.

CDK7-IN-2 is a potent inhibitor of CDK7. CDK7 is implicated in both temporal control of the cell cycle and transcriptional activity. CDK7 is implicated in the transcriptional initiation process by phosphorylation of Rbpl subunit of RNA Polymerase II (RNAPII). CDK7 has the potential for the research of cancer disease, in particular aggressive and hard- to-treat cancers (extracted from patent WO2019099298A1, compound 1).

Abemaciclib metabolite M2-d₆ is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC₅₀s in the range of 1-3 nM. Anti-cancer activity.

DB18 is a potent and selective inhibitor of CDC2-like kinases (CLKs), with IC₅₀ values in the range of 10-30 nM for CLK1, CLK2 and CLK4. DB18 has anti-tumor activity.

CDK1 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Eriocalyxin B is a diterpenoid compound that can be isolated from Chinese herb Isodon eriocalyx. Eriocalyxin B exhibits multiple activities, such as anti-cancer, anti-inflammatory, and inhibition of adipogenesis. Eriocalyxin B is capable of inducing apoptosis and autophagy in tumor cells. Eriocalyxin B can be used in the research of cancers, autoimmune diseases, and other conditions.

N9-Isopropylolomoucine is a mitotic cyclin dependent kinase (CDK) inhibitor. N9-Isopropylolomoucine targets CCNB 1/CDK1 and can be used for cancer research.

CDK2/MDM2-IN-1 (III-13) is a dual inhibitor of CDK2/MDM2 with an IC₅₀ value of 2.60 nM for CDK2. CDK2/MDM2-IN-1 has antitumor activity.

CDK2-IN-13 (Compound 15) is a CDK2 inhibitor with an IC₅₀ of 12 µM. CDK2-IN-13 can be used in research of cancer.