CDK Inhibitor

Cdk16 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk16 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

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.

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.

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.

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.

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].

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.

(R)-Roscovitine-d₇ (Seliciclib-d₇; CYC202-d₇) is deuterium-labeled (R)-Roscovitine (HY-30237).

ZSQ836 is an orally active dual covalent inhibitor of CDK12/CDK13, with an EC₅₀ value of 32 nM against CDK12. ZSQ836 can induce apoptosis and exhibit anticancer activity in vivo. ZSQ836 can be used in the study of ovarian cancer.

Samuraciclib hydrochloride (Standard) is the analytical standard of Samuraciclib hydrochloride (HY-103712A). This product is intended for research and analytical applications. Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 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.

THZ531 (Standard) is the analytical standard of THZ531 (HY-103618). This product is intended for research and analytical applications. THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC₅₀s of 158 nM and 69 nM, respectively.

CC-671 (Standard) is the analytical standard of CC-671 (HY-108709). This product is intended for research and analytical applications. CC-671 is a dual TTK protein K_inase/CDC2-like K_inase (CLK2) inhibitor with IC₅₀s of 0.005 and 0.006 μM for TTK and CLK2, respectively.

3MB-PP1 (Standard) is the analytical standard of 3MB-PP1 (HY-102069). This product is intended for research and analytical applications. 3MB-PP1, a bulky purine analog, is a Polo-like kinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC₅₀=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division.