CDK Inhibitor

Avotaciclib (BEY1107) sulfate is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib sulfate can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib sulfate can be used in the research of cancer such as pancreatic cancer and lung cancer.

MPT0L145 is a PIK3C3/FGFR inhibitor, with a K_d value of 0.53 nM for PIK3C3. MPT0L145 decreases the phosphorylation of FGFR1, FGFR3 and their downstream proteins (FRS2, ERK and Akt). MPT0L145 induces G0/G1 cell cycle arrest and decreased protein levels of cyclin E. MPT0L145 promotes mitochondrial dysfunction, ROS production, and DNA damage. MPT0L145 is an autophagy inhibitor. MPT0L145 significantly sensitizes cancer cells to targeted or chemotherapeutic agents. MPT0L145 can be used for cancer research, such as bladder cancer and NSCLC.

Cdk12 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk12 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Hsp90-IN-42 is a heat shock protein 90 (Hsp90) inhibitor with an IC₅₀ of 15.65 nM against human targets. Hsp90-IN-42 destabilizes EGFR and inhibits the activation of the EGFR-Akt signaling pathway. Hsp90-IN-42 suppresses the proliferation and migration of cancer cells, induces cell cycle arrest by downregulating CDK12 and CDK13, and triggers mild apoptosis via downregulating Bcl-2 and upregulating Bax. Hsp90-IN-42 inhibits tumor growth in xenograft mouse models. Hsp90-IN-42 can be used in research related to colorectal cancer.

Cdc7-IN-20 (EP-05) is an orally effective and selective Cdc7 inhibitor with IC₅₀ and K_i values of 0.93 and 0.11 nM, respectively. Cdc7-IN-20 has antitumor activity.

5-HT6 inverse agonist 1 (Compound 33) is an antagonist for 5-HT6 receptor with a K_i of 23 nM and a K_b of 6.62 nM. 5-HT6 inverse agonist 1 inhibits the 5-HT6R mediated Cdk5 and mTOR signaling pathway. 5-HT6 inverse agonist 1 reduces tactile hypersensitivity in spinal nerve ligation (SNL)-induced rat model.

VMY-1-101 is a fluorescent cyclin-dependent kinase (CDK) inhibitor, with an excitation of 410 nm and emission of 512 nm. VMY-1-101 competitively inhibits ATP binding to CDKs. VMY-1-101 induces G2/M cell cycle arrest in human breast cancer cells. VMY-1-101 induces modest apoptosis in human breast cancer cells. VMY-1-101 blocks proliferation of human breast cancer cells, including multidrug resistance-positive cells, and is not a substrate for p-glycoprotein. VMY-1-101 localizes to the cytoplasm of human breast cancer cells. VMY-1-101 shows increased binding to human breast cancer tissue compared to fluorophore alone. VMY-1-101 can be used for the research of breast cancer.

FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC₅₀=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo.

VEGFR2-IN-86 is a dual VEGFR2/CDK2 inhibitor, with an IC₅₀ of 0.06 μM against VEGFR2 and an IC₅₀ of 0.78 μM against CDK2. VEGFR2-IN-86 induces G-phase cell cycle arrest, reduces colony-forming ability and tumor cell migration capacity, and exerts antiproliferative activity in cancer cells. VEGFR2-IN-86 can be used for the research of breast cancer and prostate cancer.

CDK2-IN-59 is a CDK2 inhibitor with a IC₅₀ of 66.33 μM. CDK2-IN-59 stably interacts within the CDK2 active site and induces apoptosis in breast cancer cells. CDK2-IN-59 can be used for the research of breast cancer.

Isosilybin B (Standard) is the analytical standard of Isosilybin B (HY-N7045). This product is intended for research and analytical applications. Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer.

Anticancer agent 300 (compound P14) is a CCND1, CDK4, CDK6, and CCNE1 modulator, with anti-proliferative, cell-cycle modulatory, senescence-inducing, and apoptosis-inducing activity. Anticancer agent 300 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma.

HER4/HER2-IN-1 (Compound 4b) is a HER4/HER2 inhibitor. HER4/HER2-IN-1 inhibits the proliferation of HER2-positive cells. HER4/HER2-IN-1 reduces the total expression level of HER2 in A431 cells, while the phosphorylated HER2 (p-HER2) does not decrease. HER4/HER2-IN-1 lowers the level of cell cycle protein D1 (cyclin D1) and stimulates the cleavage of PARP. HER4/HER2-IN-1 can be used for the study of cancer, such as breast cancer.

CDK1-IN-4 (10d) is a selective CDK1 inhibitor with IC₅₀s of 44.52, 624.93 and 135.22 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN4 inhibits the growth of cancer cells by affecting cell cycle. CDK1-IN-4 can be used for the research of cancer.

BRD4/AKT-IN-1 is a BRD4/AKT inhibitor with BRD4 IC₅₀ 66.12 nM and AKT1 IC₅₀ 143.81 nM. BRD4/AKT-IN-1 blocks BRD4-mediated c-Myc transcriptional regulation, modulates AKT1 signaling, decouples AKT phosphorylation from pro-survival effectors. BRD4/AKT-IN-1 induces G0/G1 cell cycle arrest via downregulated phosphorylated RB, cyclin E1, CDK2. BRD4/AKT-IN-1 elevates LC3B levels to promote autophagy. BRD4/AKT-IN-1 promotes apoptosis in cancer cells. BRD4/AKT-IN-1 can be used for the research of metastatic castration-resistant prostate cancer.

Amantadine in Methanol (Standard) is the solution of Amantadine (Standard). This product is intended for research and analytical applications. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[4].

VEGFR-2-IN-69 (Compound 5A) is a dual inhibitor of VEGFR-2 and Telomerase, which upregulates the expression of caspase 3, caspase 8 and caspase 9, while downregulating CDK-2, CDK-4 and CDK-6. VEGFR-2-IN-69 exhibits an IC₅₀ of 15.46 µM against HCT116 cells.

SST0116CL1 free base is a HSP90 inhibitor (IC₅₀: 0.21 μM). SST0116CL1 free base binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 free base induces degradation of Her2 in BT-474 cell (IC₅₀: 0.2 μM). SST0116CL1 free base has antiproliferative activity and inhibits tumor growth. SST0116CL1 free base has antiproliferative activity and inhibits tumor growth. SST0116CL1 free base can be used for the study of leukemia, gastric and ovarian carcinoma.

CDK8/19-IN-2 (compound 12) is an orally active and potent cyclin-dependent kinase 8/19 (CDK8 and CDK19) inhibitor, with IC₅₀ values of 2.08 and 2.49 nM, respectively. CDK8/19-IN-2 can be used for acute myeloid leukemia (AML), breast cancer, and lymphoma research.

JNJ-7706621 (Standard) is the analytical standard of JNJ-7706621 (HY-10329). This product is intended for research and analytical applications. JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC₅₀s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.