CDK4

CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM). CDK4/6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.

CDK4/6-IN-2 is a potent inhibitor of CDK4 and CDK6 [IC50s: 2.7 and 16 nM].

CDK4/6-IN-3, a brain-penetrant CDK4/CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM), is used for the treatment of glioblastoma and inhibits CDK1 with a Ki of 110 nM.

CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectively.

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.

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.

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.

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.

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and exhibits over 1,000-fold reduced potency against the cyclin B/CDK1 complex.

Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor (IC50:10/39 nM).

Rafoxanide as a dual CDK4/6 inhibitor for the treatment of skin cancer. Rafoxanide is a salicylanilide used as an anthelmintic. It is used to treat fluke, hookworm and other infestations.

PU02 (6-[(1-Naphthalenylmethyl)thio]-9H-purine) is a potent and selective antagonist of 5-HT3 receptor.

LSN2839567 (Abemaciclib metabolite M2) is the active metabolite of Abemaciclib, a potent CDK4 and CDK6 inhibitor (IC50s: 1-3 nM) with anticancer activity.LSN2839567 inhibits CDK9.LSN2839567 inhibits cell growth and cell cycle progression in a concentration-dependent manner. cell growth and cell cycle progression in a concentration-dependent manner and can be used to study breast and lung cancer.

Lerociclib (G1T38) is a selective and highly potent CDK4/6 inhibitor with anticancer and antitumor activity, inhibits CDK4/CyclinD1 and CDK6/CyclinD3, and inhibits tumor growth in an animal model of endocrine-resistant breast cancer. Due to the poor solubility, for animal studies, the salt form T11345L is recommended.

MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.

Trilaciclib is a short-acting, orally effective CDK4/6 inhibitor with IC₅₀ values of 1 nM and 4 nM respectively. It transiently and reversibly induces G1 cell cycle arrest, mitigates chemotherapy-induced myelosuppression, and enhances antitumour immunity, making it applicable across multiple cancers.

XY028-133 is a PROTAC-based CDK4/6 degrader for the study of tumors.

AG-024322 is a potent ATP-competitive inhibitor targeting pan-CDK, effectively inhibiting cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range (1-3 nM).

CDKI-73 is a potent CDK9 inhibitor (Ki: 4 nM). It shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).The inhibition of CDK9 induces apoptosis and potentiates the effect of cisplatin.

Ribociclib hydrochloride (LEE011 HCl) is a selective, orally active cyclin-dependent kinase CDK4/6 inhibitor (IC50=10/39 nM) that blocks cell cycle progression and inhibits tumor cell proliferation.

Ribociclib succinate hydrate is a highly specific CDK4/6 inhibitor (IC50s: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.