CDK6 Inhibitor

Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

Cimpuciclib is a selective CDK4 inhibitor (IC₅₀: 0.49 nM) that has anti-tumor activity.

CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with K_is of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a K_i of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma.

Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC₅₀s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib shows antitumor activity on cisplatin-resistant cells.

CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC₅₀ values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively.

CDK7-IN-30 (Compound 22) is a CDK7 inhibitor (IC₅₀ = 7.21 nM) that effectively inhibits the phosphorylation of RNA Polymerase II and CDK2. CDK7-IN-30 CDK7-IN-30 can induce cell apoptosis and has anti-cancer activity and can be used in cancer research.

CDK4/6-IN-23 (Compound 42) is a potent and selective CDK4/6 inhibitor, with an IC₅₀ of 11 nM for CDK6. CDK4/6-IN-23 can significantly activate immune cells and promote the production of IL-3. CDK4/6-IN-23 has dual myeloprotective and immunomodulatory effects in 5-FU (HY-90006) chemotherapy mice.

CDK4/6-IN-28 is a potent, orally active, and selective CDK4/6 inhibitor IC₅₀ values of 14.02 and 10.03 nM, respectively. CDK4/6-IN-28 inhibits breast cancer cell colony formation, migration, and proliferation. CDK4/6-IN-28 induces G1-phase cell cycle arrest and apoptosis in breast cancer cells. CDK4/6-IN-28 exhibits tumor inhibitory activity in breast cancer xenograft mouse models. CDK4/6-IN-28 can be used for the research of breast cancer.

CDK4/6-IN-7 is a potent, selective and orally active CDK4/6 inhibitor, with IC₅₀s of 1.58 and 4.09 nM, respectively. CDK4/6-IN-7 can be used for the research of breast cancer.

PF-06842874 is a CDK4/Cyclin D1 and CDK6/Cyclin D3 inhibitor (K_i values are 62 and 130 nM, respectively). PF-06842874 can be used in the research of pulmonary arterial hypertension and cancer.

LCI133 is afirst-in-class,nanomolar-potent, selective multikinase inhibitor targeting CDK4/6/9 and AURKA/B (IC₅₀ = 4.7/10.2/4.1 nM and 2.8/10.6 nM). LCI133 induces S/G2 cell-cycle arrest and robust apoptosis in MYCN-amplified neuroblastoma BE(2)-C cells. LCI133 demonstrates significant antitumor efficacy in a BE(2)-C neuroblastoma xenograft model.

CDK6-IN-2 is a CDK6 covalent inhibitor with an IC₅₀ of 0.013 μM. CDK6-IN-2 inhibits the proliferation and migration of triple-negative breast cancer cells, and induces cell cycle arrest and apoptosis. CDK6-IN-2 induces ROS accumulation and mitochondrial damage through cellular metabolic reprogramming. CDK6-IN-2 exhibits anti-tumor activity and can be used for the research of triple-negative breast cancer.

CDK4/6-IN-21 maleate (compound I-52) is a CDK4/6 inhibitor with IC₅₀ values of 3.88 and 3.31 nM for CDK4 and CDK6, respectively. CDK4/6-IN-21 maleate has antitumor activity.

CDK4/6-IN-20 (Compound II-5) is a CDK4/CDK6 inhibitor with IC₅₀ values ​​of 1.9, 14.2 nM, respectively. CDK4/6-IN-20 also inhibits cell proliferation and can be used in cancer research.

Palbociclib-C4-Boc is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for CDK4/6 Palbociclib (HY-50767) and a PROTAC linker (HY-W007803), which recruits E3 ligases. Palbociclib-C4-Boc can be used for synthesis of PROTAC BSJ-03-204 (HY-136250).

G721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer.

CDK2/4/6-IN-1(example 29) is a CDK2/4/6 inhibitor with IC₅₀ values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research. CDK2/4/6-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

PB1-3 is an orally active CDK4/CDK6 inhibitor with selective antiproliferative activity against 4T1 and MCF-7 breast cancer cells. PB1-3 directly binds to CDK4 and CDK6, downregulates total protein expression, reduces Rb phosphorylation, and induces G0/G1 phase arrest. PB1-3 induces ROS accumulation, mitochondrial membrane potential collapse, initiation of mitochondria-mediated intrinsic apoptosis, upregulation of the Bax/Bcl-2 ratio, and activation of cleaved caspase-3. PB1-3 inhibits tumor growth in a 4T1 orthotopic syngeneic mouse model. PB1-3 can be used for research related to triple-negative breast cancer.

CDK4/6-IN-29 is an orally active and highly selective CDK4/6 inhibitor, with an IC₅₀ of 3.17 nM against CDK4 and an IC₅₀ of 4.91 nM against CDK6. CDK4/6-IN-29 induces apoptosis in non-small cell lung cancer cells, inhibits cancer cell migration, induces G1-phase cell cycle arrest, and exhibits anti-tumor efficacy in vivo. CDK4/6-IN-29 can be used for research related to non-small cell lung cancer.