cyclin b1

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

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.

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.

H1k is an eudistomin Y fluorescent derivative and lysosome-targeted antiproliferative agent that dose-dependently increases autophagy signalling and down-regulates the expression of cyclin-dependent kinase (CDK1) and cyclin B1.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK/p38 MAPK signaling pathways in the murine macrophages.

MAPK-IN-3 (Compound 4a) is an antiproliferative agent demonstrating significant inhibitory effects on KYSE 30, HCT 116, and HGC 27 cell lines, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. This compound arrests the cell cycle via a p53-dependent mechanism and induces apoptosis through a p53-independent pathway. It reduces the expression of cell cycle-related proteins, such as Cyclin D1 and Cyclin B1, while increasing pro-apoptotic proteins like cleaved PARP, cleaved caspase-7, and cleaved caspase-9. MAPK-IN-3 also decreases anti-apoptotic proteins such as Bcl-2, elevates ROS levels in KYSE 30 cells, and enhances the expression of ROS-related MAPK pathway members, including p-ERK, p-p38, and p-JNK.

Sutopin-2 is a topoisomerase II inhibitor that affects cell cycle progression and microtubule stability. It induces cell cycle arrest by regulating the nuclear-cytoplasmic transport of cyclin B1.

SH514 is a specific IRF4 inhibitor with an IC₅₀ of 2.63 µM, binding to the DNA-binding domain (IRF4-DBD) of IRF4 to block its transcriptional activity and inhibit the expression of downstream genes such as CCNC, CANX, E2F5, CMYC, HK2, and Blimp1, and inhibits the expression of MM cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC, making it useful for studying multiple myeloma and malignant haematological diseases.

Anticanceragent 264 (Compound 5w) is an anticancer compound that exhibits significant antiproliferative activity in tumor cell lines, with an IC50 range of 7.5-33.67 μM. It notably induces cell cycle arrest at the G2/M phase in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines. This compound reduces key cell cycle proteins CDK1, CDK2, and Cyclin B1 in a dose-dependent manner and has strong binding activity with differentiation inhibitors and DNA-binding proteins. Anticanceragent 264 is useful for research in the cancer disease domain.

CDC20-IN-2 (14c) is an inhibitor of Cdc20 with a KD of 7.65 μM, inducing G2/M phase arrest, promoting DNA damage accumulation, and stabilizing key substrates such as Cyclin B1 and Bim. This leads to enhanced apoptosis, as well as inhibition of tumor cell proliferation and migration.

Antitumor agent-174 (Compound 10) directly binds to the N-terminal site of Hsp90, promoting the degradation of β-catenin and thereby inhibiting Wnt/β-catenin signaling. This compound effectively suppresses the proliferation of colorectal cancer (CRC) cells, induces S and G2/M phase arrest, and prevents cell colony formation. It downregulates proteins such as CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, while upregulating P21. Antitumor agent-174 exhibits significant antitumor activity against CRC, offering excellent pharmacokinetics and low toxicity.

RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

MPT0B206 is a novel tubulin polymerization inhibitor. MPT0B206 induced G2/M cell cycle arrest and the appearance of the mitotic marker MPM-2 in K562 and K562R cells, which is associated with the upregulation of cyclin B1 and the dephosphorylation of Cdc2.

Olomoucine II is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 7.6, 0.1, 19.8, 0.45, and 0.06 μM for Cdk1, -2, -4, -7, and -9, respectively).1It is selective for CDKs over 10 additional kinases (IC50s = >100 μM for all) but does inhibit ERK2 (IC50= 32 μM) and the ATP-binding cassette transporter B1 (ABCB1; IC50= 6.4 μM).1,2Olomoucine II inhibits proliferation of a variety of cancer cells, including those expressing wild-type p53 or mutant p53 (mean IC50s = 7.4 and 10.1 μM, respectively), and it acts synergistically with daunorubicin to inhibit proliferation of HCT-8 cells that endogenously express ABCB1. Olomoucine also inhibits replication of herpes simplex virus 1 (HSV-1), HSV-2, vaccinia virus, human adenovirus type 4 (Ad4), and human CMV (IC50s = 5, 4.7, 3.8, 2.4, and 3.2 μM, respectively) but not measles virus or influenza virus (IC50s = >20 μM for both).3

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cd

Cucurbitacin E is a natural product isolated from the climbing stem of Cucumic melo L. It significantly suppresses the activity of the cyclin B1/CDC2 complex.Cucurbitacin E has prevention of neurodegeneration, it has potent anti-proliferative, antineoplas

LG308 shows antimicrotubule activity which is a novel synthetic compound. LG308 induces apoptosis, cell death, and significantly suppresses tumor growth that has the potential for the prostate cancer research. LG308 induces arrest of mitotic phase and significantly inhibits progression of G2/M which is associated with the upregulation of cyclin B1 and mitotic marker MPM-2 and the dephosphorylation of cdc2 [1].

p53 Activator 2 (compound 10ah) intercalates into DNA, causing significant double-strand breaks and upregulating the expression of p53, p-p53, CDK4, and p21, leading to cell cycle arrest at the G2/M phase. It induces apoptosis, reduces anti-apoptosis proteins Bcl-2, Bcl-xL, and cyclin B1 levels, and shows anti-proliferative activity against MGC-803 cells with an IC50 of 1.73 μM. Additionally, p53 Activator 2 exhibits potent anticancer effectiveness in MGC-803 xenograft tumor models [1].

DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -treatment in HT-1080 cells resulted in microtubule de-polymerization and G2/M phase arrest preceding apoptosis. Phosphor-cdc2 (thr14/tyr15) reduction, cyclin B1 accumulation and aberrant spindles denoted the cyclin B1-cdc2 complex active and M phase arrest in HT-1080 cells treated with DAT-230. Apoptosis induced by DAT-230 was related with the activation of caspase-9, caspase-3 and PARP cleavage, which were at the downstream of mitochondria.

MPT0B214 is a novel and potent microtubule inhibitor with potential anticancer activity. MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin's colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of the mitotic marker MPM-2. Furthermore, the compound induced apoptotic cell death through mitochondria/caspase 9-dependent pathway. Notably, several KB-derived multidrug-resistant cancer cell lines were also sensitive to MPT0B214 treatment. ( PLoS One. 2013;8(3):e58953).

RGB-286638 is a multi-target CDK inhibitor that effectively hampers the kinase activity of a range of cyclin-CDK complexes, including cyclin T1-CDK9 (IC50 = 1 nM), cyclin B1-CDK1 (IC50 = 2 nM), cyclin E-CDK2 (IC50 = 3 nM), cyclin D1-CDK4 (IC50 = 4 nM), cyclin E-CDK3 (IC50 = 5 nM), and p35-CDK5 (IC50 = 5 nM). Additionally, it inhibits other kinases such as GSK-3β (IC50 = 3 nM), TAK1 (IC50 = 5 nM), Jak2 (IC50 = 50 nM), and MEK1 (IC50 = 54 nM), showcasing its versatile inhibitory potential.

CDK2-IN-27 (compound 1) is an effective inhibitor of CDK2, exhibiting IC50 values of <10 nM for CDK2/cyclin E1 and >10-20 nM for CDK2/cyclin B1, respectively [1].

PLK1-IN-10 (Compound 4Bb), an orally active inhibitor of the PLK1 PBD (polo-box domain), inhibits the interaction between PLK1 and the cell division regulator protein 1 (PRC1) and reduces the protein expression of the CDK1-Cyclin B1 complex. Additionally, PLK1-IN-10 interacts with glutathione (GSH), enhancing cellular oxidative stress and promoting cell death [1].

Akt/mTOR-IN-1 (Compound 8r) is an inhibitor of the AKT/mTOR signaling pathway, exhibiting an IC50 of 0.8 µM and possessing anticancer activity. This compound decreases the expression of Caspase 3 while enhancing the expression of the autophagic protein Cyclin B1, thereby inducing autophagy and apoptosis. Akt/mTOR-IN-1 is applicable for research in the field of non-small cell lung cancer (NSCLC).