cyclin-d1

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.

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

Compound SC-1 is a a derivative of the multiple tyrosine kinase inhibitor sorafenib. Compound SC-1 potently inhibits the phosphorylation of STAT3 by blocking STAT3 phosphorylation and activation, and induces apoptosis in hepatocellular carcinoma cell lines[1].

Briciclib (ON 014185) is a small molecule that inhibits cyclin D1 accumulation in Y cells.

KPT-6566 is a novel selective covalent pin1 inhibitor, KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain,and has anti-cancer activity.

DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].

Eurycomalactone is a natural product isolated from Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor( IC50 of 0.5 μM). Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα/β and IκBα.

FIDAS-3, a stilbene derivative and potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A), exhibits anticancer activities by effectively competing with S-adenosylmethionine (SAM) for MAT2A binding.

FIDAS-5 is an orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. It can effectively compete with S-adenosylmethionine for MAT2A binding and has anticancer effects.

Salidroside is a bioactive phenolic glycoside compound isolated from Rhodiola rosea and is a prolyl endopeptidase inhibitor. Salidroside can alleviate cachexia symptoms in a tumor cachexia mouse model by activating mTOR signaling and protect dopaminergic neurons by enhancing PINK1/Parkin-mediated mitochondrial autophagy. Salidroside can also inhibit the growth of cancer cells by regulating the CDK4-cyclin D1 pathway to block the G1 phase and/or regulating the Cdc2-cyclin B1 pathway to block the G2 phase.

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

LOM612 is a potent and specific FOXO relocator that induces nuclear translocation of the FOXO3a reporter protein as well as endogenous FOXO3a and FOXO1 in a dose-dependent manner in U2OS cells, down-regulates the expression of c-Myc and cyclin D1, and has anti-proliferative effects in human cancer cell lines.

GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

Rubone (2'-Hydroxy-2,4,4',5,6'-pentamethoxychalcone), a natural product and a modulator of miR-34a (microRNA-34), upregulates miR-34a expression in a p53-dependent manner, which in turn downregulates the expression of downstream targets Bcl-2, cyclin-D1, CDK6, SIRT1, and FOXP1, thereby inhibiting tumor growth and reversal of hepatocellular carcinoma (HCC) and chemoresistance in prostate cancer.

Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

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.

Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective CDK4/CDK6 inhibitor, with IC50 values of 2 nM for CDK6/CyclinD3 and 1 nM for CDK4/CyclinD1.

Indirubin-5-sulfonate shows inhibitory activity against GSK-3β. Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1,

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.

Palbociclib-d8 (PD 0332991 D8) is the 2H-labeled form of Palbociclib. Palbociclib is an orally active CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM). Palbociclib has anti-tumor activity and is used in research for estrogen receptor-positive and HER2-negative breast cancer.

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

Trilaciclib hydrochloride (G1T28 hydrochloride) is an inhibitor of CDK4/6 (IC50s: 1 nM and 4 nM for CDK4 and CDK6).