Catalog No.
Product Name
Application
Product Information
Citations
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Casein Kinase inhibitor
BTX-A51 (Casein Kinase Inhibitor A51) is a potent, orally bioavailable inhibitor of casein kinase 1α (CK1α). It effectively induces apoptosis in leukemia cells and demonstrates strong anti-leukemic activity in preclinical models, making it a promising therapeutic candidate for hematologic malignancies. -
PROTAC CDK12-Cyclin K degrader
PP-C8 is a potent and selective PROTAC degrader targeting the CDK12–Cyclin K complex. It induces efficient degradation of CDK12 and Cyclin K with DC₅₀ values of 416 nM and 412 nM, respectively. In preclinical models, PP-C8 exhibits strong synergistic antiproliferative effects when combined with PARP inhibitors, particularly in triple-negative breast cancer (TNBC), highlighting its potential as a therapeutic strategy for enhancing DNA damage response–targeted treatments. -
PROTAC CDK12/13 Degrader
PROTAC CDK12/13 Degrader-1 (7f) is a highly selective dual degrader targeting CDK12 and CDK13, with DC₅₀ values of 2.2 nM and 2.1 nM, respectively. It exhibits potent anti-proliferative activity and serves as a valuable tool for investigating transcriptional regulation and therapeutic strategies in breast cancer research. -
PROTAC CDK8-cyclin C dual degrader
LL-K8-22 is a potent, selective, and durable PROTAC degrader targeting the CDK8–cyclin C complex, with DC₅₀ values of 2.52 μM and 2.64 μM, respectively. It suppresses STAT1 Ser727 phosphorylation and inhibits E2F- and MYC-driven oncogenic transcriptional programs. LL-K8-22 shows potential for use in triple-negative breast cancer (TNBC) research and related therapeutic studies. -
PROTAC CDK4/6 Degrader
XY028-133 (Example 14) is a PROTAC-based degrader targeting CDK4/6, composed of ligands for von Hippel-Lindau (VHL) and CDK. It induces selective degradation of CDK4/6 and exhibits anti-tumor activity, making it a useful tool for cell cycle and cancer research. -
PROTAC CDK4/6 Degrader
BSJ-03-204 triTFA is a potent and selective PROTAC degrader targeting CDK4/6, constructed using ligands for cereblon and CDK. Based on Palbociclib, it exhibits IC₅₀ values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and shows anti-cancer activity, making it a valuable tool for cell cycle and oncology research. -
PROTAC CDK12/13 Degrader
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective dual degrader of CDK12 and CDK13, with DC₅₀ values of 2.2 nM and 2.1 nM, respectively. It exhibits strong antiproliferative activity and is a valuable tool for investigating cell cycle regulation and therapeutic strategies in breast cancer research. -
PROTAC CDK12 Degrader
BSJ-4-116 is a PROTAC molecule derived from a modified form of the multi-kinase degrader TL12-186, linked to a cereblon ligand and E3 ligase ligand intermediate. It induces time- and concentration-dependent degradation of CDK12 in Jurkat T cells and downregulates genes involved in DNA double-strand break repair at 50 nM. BSJ-4-116 also inhibits MOLT-4 leukemia cell growth in a cereblon-dependent manner, supporting its application in cancer and DNA repair research. -
PROTAC CDK2/9 Degrader
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual PROTAC degrader targeting CDK2 (DC₅₀ = 62 nM) and CDK9 (DC₅₀ = 33 nM), constructed by linking a CDK inhibitor to a cereblon ligand. It effectively inhibits PC-3 prostate cancer cell proliferation (IC₅₀ = 0.12 µM) by inducing cell cycle arrest in the S and G2/M phases, making it a valuable tool for cancer and cell cycle research. -
PROTAC CDK4 Degrader
BSJ-04-132 is a potent and selective Ribociclib-based PROTAC degrader targeting CDK4, constructed using ligands for cereblon and CDK. It exhibits IC₅₀ values of 50.6 nM for CDK4/D1 and 30 nM for CDK6/D1, while sparing CDK6 and IKZF1/3 from degradation. BSJ-04-132 demonstrates anti-cancer activity and is a valuable tool for cell cycle and oncology research. -
PROTAC CDK4/6 Degrader
BSJ-03-204 is a potent and selective PROTAC degrader targeting CDK4 and CDK6, constructed by linking Palbociclib to a cereblon ligand. It exhibits IC₅₀ values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1, without inducing degradation of IKZF1 or IKZF3. BSJ-03-204 demonstrates strong anti-cancer activity and is a valuable tool for cell cycle and oncology research. -
multi-kinase PROTAC degrader
TL12-186 is a cereblon-dependent PROTAC degrader with broad-spectrum activity against multiple kinases, including CDKs, BTK, FLT3, Aurora kinases, TEC, ULK, and ITK. It inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC₅₀ values of 73 nM and 55 nM, respectively, making it a valuable tool for studying kinase-driven signaling pathways and cancer biology. -
PROTAC CDK4/6 degrader
XY028-140 (MS140) is a highly potent and selective dual-function compound that acts as both a CDK4/6 kinase inhibitor and a PROTAC degrader. By combining kinase inhibition with targeted protein degradation, MS140 provides an effective approach for disrupting CDK4/6-mediated cell cycle regulation, making it a valuable tool for cancer research. -
CDK6-degrading PROTAC
YX-2-107 is a CDK6-degrading PROTAC with an IC50 of 4.4 nM, designed for selective degradation of CDK6. This compound effectively inhibits retinoblastoma (RB) phosphorylation and reduces FOXM1 expression in vitro. YX-2-107 has potential applications in research related to Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), demonstrating its ability to attenuate disease progression in rat models. -
CDK2 Degrader
CPS2 is a highly potent and selective PROTAC that irreversibly degrades cyclin-dependent kinase 2 (CDK2) with an IC50 of 24 nM. This compound is valuable for exploring the role of CDK2 in cell cycle regulation and has applications in the study of acute myeloid leukemia. Its unique mechanism provides a powerful tool for researchers investigating targeted protein degradation in cancer therapies. -
PROTAC CDK6 Degrader
CP-10 is a PROTAC designed to selectively target and degrade cyclin-dependent kinase 6 (CDK6) through its binding to Cereblon. Demonstrating a DC50 of 2.1 nM, this compound effectively inhibits the proliferation of various hematopoietic cancer cell lines, including multiple myeloma, and is capable of degrading both mutated and overexpressed forms of CDK6. Its specific activity makes CP-10 a valuable tool for research into CDK6-related malignancies and potential therapeutic strategies. -
PROTAC Degrader
SNX7886 is a potent PROTAC degrader targeting CDK8 and CDK19. It effectively induces degradation of CDK8 and CDK19, achieving up to 90% and 80% degradation, respectively, in 293 cells. This compound is valuable for research applications in understanding the role of CDK8/19 in various biological processes and cancer pathways. -
Kinases PROTAC
DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions. -
PROTAC CDK4/6 Degrader
BSJ-02-162 is a potent PROTAC degrader targeting CDK4/6 through the utilization of a thalidomide-based E3 ligase ligand and a selective CDK4/6 inhibitor. This compound effectively recruits ubiquitin ligases to facilitate the targeted degradation of CDK4/6, thereby modulating cellular responses to cell cycle regulation. BSJ-02-162 is designed for research applications exploring cancer therapies and the mechanisms of protein homeostasis within tumor cells. -
CDK2 molecular glue Degrader
CDK2 degrader 1 is a selective molecular glue degrader targeting cyclin-dependent kinase 2 (CDK2). It effectively induces ubiquitination and proteasomal degradation of CDK2 by binding to cereblon, achieving a Dmax greater than 80% and a Ki greater than 1 μM. This compound is utilized in cancer research, providing insights into tumor biology and potential therapeutic strategies. -
CDK Inhibitor
(S)-CR8 is a selective inhibitor of cyclin-dependent kinases (CDKs), demonstrating potent inhibitory activity with IC50 values of 0.060 μM for CDK2/cyclin E, 0.080 μM for CDK2/cyclin A, 0.11 μM for CDK9/cyclin T, 0.12 μM for CDK5/p25, and 0.15 μM for CDK1/cyclin B. This compound effectively reduces the survival of SH-SY5Y cells, with an IC50 of 0.40 μM, making it a valuable tool for studying cell cycle regulation and potential therapeutic strategies in cancer research. -
CDK Inhibitor
Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders. -
CDK Inhibitor
NSC693868 is a selective inhibitor of cyclin-dependent kinases CDK1 and CDK5, demonstrating IC50 values of 600 nM and 400 nM, respectively. This compound also exhibits weaker inhibition of GSK3β with an IC50 of 1 µM and does not affect CDC25 activity. NSC693868 is employed in research to elucidate the functions of CDK1 and CDK5 within various cellular signaling pathways. -
GSK-3α/β Inhibitor
(E/Z)-BIO-acetoxime is a potent and selective inhibitor of GSK-3α/β, exhibiting an IC50 of 10 nM. This compound demonstrates exceptional selectivity with over 200-fold preference against CDK5/p25, CDK2/cyclin A, and CDK1/cyclin B, with IC50 values of 2.4, 4.3, and 63 μM, respectively. Its strong inhibitory activity makes it a valuable tool for research focused on signaling pathways involved in cell proliferation, differentiation, and apoptosis. -
CDK9 Inhibitor
Tambiciclib is a potent and selective CDK9 inhibitor with an IC50 of 1 nM, exhibiting over 200-fold selectivity against other cyclin-dependent kinases and significant selectivity over DYRK1A/B and a wide range of kinases. This compound has demonstrated effective in vitro and in vivo antileukemic activity in acute myeloid leukemia (AML) models by inhibiting RNA Polymerase II phosphorylation, leading to downregulation of MCL1 and MYC, and subsequent induction of apoptosis. Tambiciclib is suitable for research applications focused on AML and related oncological studies. -
Cyclin/CDK Inhibitor
VMY-1-103 is a selective inhibitor of the cyclin-dependent kinase (CDK) complex, effectively arresting the cell cycle at the G1 phase. It has been demonstrated to reduce mitochondrial membrane potential, induce p53 phosphorylation, and trigger PARP cleavage, ultimately activating caspase-3 and initiating apoptosis in LNCaP prostate cancer cells. This compound is valuable for research applications focused on cancer biology and the mechanisms of cell cycle regulation and apoptosis. -
CDK2/4/6 PROTAC Degrader
PROTAC CDK2/4/6 Degrader-2 is a targeted protein degradator specifically designed to degrade cyclin-dependent kinases CDK2, CDK4, and CDK6. This compound effectively inhibits cell proliferation and induces cell cycle arrest and apoptosis in malignant melanoma cells. Its application extends to cancer research, particularly in investigating the role of CDK2/4/6 in tumor biology. The compound can also be converted into its prodrug form, enabling versatile utilization in various assays related to cancer therapeutics. -
KDM1/CDK1 Inhibitor
KDM1/CDK1-IN-1 is a potent inhibitor of both KDM1 and CDK1, exhibiting IC50 values of 0.096 μM and 0.078 μM, respectively. This compound effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis in HOP-92 cancer cells. Additionally, KDM1/CDK1-IN-1 demonstrates significant cytotoxic effects against a range of cell lines, including CCRF-CEM, HOP-92, and Hep-G2, with IC50 values of 16.34 μM, 3.45 μM, and 7.79 μM, respectively. Its ability to target critical regulators of the cell cycle makes KDM1/CDK1-IN-1 valuable for cancer research applications. -
CDK1 Inhibitor
Albanol B is a selective inhibitor of Cyclin-dependent kinase 1 (CDK1), derived from arylbenzofuran. This compound demonstrates significant potential in cancer research by inhibiting cell proliferation and down-regulating CDK1 expression, leading to G2/M cell cycle arrest and apoptosis in cancer cells. Additionally, Albanol B exhibits anti-Alzheimer's activity, antibacterial properties, and antioxidant effects, while also inducing mitochondrial reactive oxygen species (ROS) production and enhancing phosphorylation levels of AKT and ERK1/2. -
HDACs/CDKs Dual Inhibitor
CDK/HDAC-IN-3 is a dual inhibitor targeting histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs). It exhibits potent and selective activity, with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM against CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3, respectively. This compound is particularly relevant for research in acute myeloid leukemia (AML), providing insights into therapeutic strategies for this disease. -
CDK Inhibitor
Ryuvidine is a selective inhibitor of cyclin-dependent kinases (CDKs), specifically targeting SET domain-containing protein 8 (SETD8) with an IC50 of 0.5 µM, thereby suppressing the monomethylation of histone H4 at lysine 20 (H4K20). Additionally, Ryuvidine inhibits CDK4 with an IC50 of 6.0 µM and KDM5A, leading to the blockade of DNA synthesis. Its biological activity includes anticancer effects against various tumor types, including breast cancer, and it also demonstrates potential therapeutic benefits in arthritis research. -
CDK9/EZH2 Dual-target Inhibitor
CDK9/EZH2-IN-1 is a dual-target inhibitor designed to inhibit both CDK9 and EZH2, exhibiting IC50 values of 83.9 nM and 108.6 nM, respectively. This compound demonstrates significant biological activity by inducing apoptosis and causing DNA double-strand breaks (DSBs). It effectively inhibits the proliferation of various cancer cell lines, including MKN45, MDA-MB-453, and SW620, with IC50 values of 136.3 nM, 171.3 nM, and 315.7 nM, respectively. CDK9/EZH2-IN-1 is suitable for research applications in understanding cancer cell biology and therapeutic development. -
cyclin D1 Inhibitor
Dehydrozingerone is a cyclin D1 inhibitor derived from ginger, known for its ability to downregulate cyclin D1 expression and induce G1 phase cell cycle arrest. This compound effectively reduces the proliferative capacity of castration-resistant prostate cancer cells in vitro and inhibits subcutaneous tumor growth by targeting cell proliferation and angiogenesis. Additionally, dehydrozingerone demonstrates notable antibacterial and antifungal properties, making it suitable for research into castration-resistant prostate cancer, bacterial infections, and food spoilage due to fungal infections. -
cyclin D1/CDK4 Inhibitor
Arcyriaflavin A is an indolo[2,3-a]carbazole compound that primarily acts as a cyclin D1/CDK4 inhibitor. This compound, derived from the marine ascidian Eudistoma sp. and the slime mold Arcyria denudata, demonstrates significant biological activity in regulating the cell cycle. Arcyriaflavin A is particularly relevant for research applications focusing on colon and lung cancer, providing insights into tumor growth and potential therapeutic strategies. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-2 is a potent inhibitor targeting EGFR, HER2, and CDK9, exhibiting IC50 values of 145.35 nM, 129.07 nM, and 117.13 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to concurrently inhibit these kinases positions it as a promising candidate for studies focused on targeted therapy and oncogenic signaling pathways. -
EGFR/HER2/CDK9/COX-2 Inhibitor
CDK9-IN-41 is a potent inhibitor of CDK9, EGFR, HER2, and COX-2, exhibiting IC50 values of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM respectively. This compound demonstrates significant antitumor activity across various cancer cell lines, including leukemia, colon, melanoma, ovarian, and breast cancer. It serves as a valuable tool for exploring the role of these kinases in cancer biology and therapeutic applications. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-3 is a potent inhibitor targeting EGFR, HER2, and CDK9, exhibiting IC50 values of 191.08 nM, 132.65 nM, and 113.98 nM, respectively. This compound demonstrates significant antitumor activity, making it valuable for research in cancer therapies and signaling pathways involving these targets. Its inhibitory effects on cell proliferation in cancer models may aid in the understanding and development of targeted treatment strategies. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-1 is a highly active inhibitor of EGFR, HER2, and CDK9, displaying IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively. This compound demonstrates significant antitumor properties, making it a valuable tool for cancer research. Its ability to target multiple kinases involved in cell proliferation and survival pathways supports investigations into therapeutic strategies for various malignancies. -
EGFR/CDK-2 Inhibitor
EGFR/CDK2-IN-1 is an inhibitor targeting both the epidermal growth factor receptor (EGFR) and cyclin-dependent kinase 2 (CDK2). This compound exhibits significant cytotoxicity against breast cancer MCF7 cells and liver cancer HepG2 cells, making it a valuable tool in cancer research. Its dual inhibition profile allows for exploration of synergistic effects in therapeutic strategies targeting these critical pathways in cancer proliferation and survival. -
CDK9/PARP Inhibitor
CDK9/PARP-IN-1 is a potent inhibitor of CDK9 and PARP1, demonstrating IC50 values of 118 nM and 107 nM, respectively. This dual inhibition results in significant antiproliferative effects across various cancer cell lines, making it a valuable tool for cancer research. CDK9/PARP-IN-1 is particularly relevant for studies investigating the therapeutic potential of targeting these pathways in oncology. -
PARP1/CDK12 Inhibitor
Antitumor agent-104 is a potent inhibitor of PARP1 and CDK12, targeting critical pathways in DNA damage repair in tumors. By inhibiting PARP1 enzymatic activity, it effectively reduces PAR protein levels, thus impairing the cellular mechanisms that protect tumor cells. This compound serves as a valuable tool in cancer research, especially in studies focused on understanding tumor biology and exploring novel therapeutic strategies. -
CDK-1/PARP-1 Inhibitor
UNPD139734 is a potent inhibitor of Cyclin-Dependent Kinase 1 (CDK-1) and Poly (ADP-ribose) polymerase 1 (PARP-1), forming stable complexes with both target proteins. This compound serves as a valuable lead for the structural optimization of dual-target anticancer agents, particularly in the context of breast cancer research. Its dual inhibition mechanism offers a promising avenue for investigating novel therapeutic strategies in oncology. -
CDK9-cyclin T1 Degrader
LL-K9-3 is a small-molecule degrader specifically targeting the CDK9-cyclin T1 complex. This compound exhibits significant anti-proliferative and pro-apoptotic activities, effectively inhibiting downstream signaling pathways associated with CDK9 and androgen receptor (AR). LL-K9-3 is particularly relevant for research involving oncogenic transcriptional programs driven by AR and Myc, making it a valuable tool in cancer studies. -
CDK6/PIM1 Inhibitor
CDK6/PIM1-IN-1 hydrochloride is a potent dual inhibitor targeting CDK6 and PIM1, exhibiting IC50 values of 39 nM and 88 nM, respectively, along with significant inhibition of CDK4 (IC50=3.6 nM). This compound effectively inhibits the proliferation of acute myeloid leukemia (AML) cells, induces G1 phase cell cycle arrest, and promotes apoptosis. CDK6/PIM1-IN-1 hydrochloride is a valuable tool for research investigating the role of CDK6 and PIM1 in cancer biology, particularly in the context of AML. -
CDK1/Cyc B Inhibitor
CDK1/Cyc B-IN-1 is a selective inhibitor of the CDK1/cyclin B complex, demonstrating an IC50 of 97 nM. This compound effectively induces apoptosis and facilitates G2/M phase cell cycle arrest, making it a valuable tool for studying cell proliferation. CDK1/Cyc B-IN-1 exhibits broad-spectrum cytotoxic activity against various cancer cell lines, supporting its potential in cancer research applications. -
CDK/CRK Inhibitor
RGB-286147 is a selective ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and CDK-related kinases (CRKs), exhibiting IC50 values between 9 to 839 nM. This compound demonstrates minimal activity against non-CDK/CRK kinases. RGB-286147 induces apoptosis in cancer cells and shows significant anti-tumor effects, making it a valuable tool for research in cancer biology and therapeutic development targeting CDK pathways. -
CDK4/6 Degrader
LA-CB1 is a CDK4/6 degrader that promotes the degradation of cyclin-dependent kinases 4 and 6 through the ubiquitin-proteasome pathway. This action disrupts the CDK4/6-Cyclin D1-Rb-E2F signaling axis, leading to G0/G1 cell cycle arrest and apoptosis. LA-CB1 demonstrates potent anti-proliferative effects against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition, cell migration, invasion, and angiogenesis. In models of triple-negative breast cancer, LA-CB1 significantly inhibits tumor growth in a dose-dependent manner, making it a valuable compound for research in breast cancer therapeutics. -
CDK6/PIM1 Inhibitor
CDK6/PIM1-IN-1 is a potent dual inhibitor targeting CDK6 and PIM1, with IC50 values of 39 nM and 88 nM, respectively, and an additional inhibition of CDK4 at an IC50 of 3.6 nM. This reagent significantly inhibits the proliferation of acute myeloid leukemia (AML) cells, induces G1 phase cell cycle arrest, and promotes apoptosis. CDK6/PIM1-IN-1 demonstrates strong anti-AML activity, making it a valuable tool for research in cancer biology and therapeutic development. -
CDK Inhibitor
1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC is a cyclin-dependent kinase (CDK) inhibitor that plays a crucial role in cancer research. This compound induces apoptosis and effectively inhibits the proliferation of a variety of cancer cell lines, making it a valuable tool for studying cancer biology and therapeutic responses. Its ability to impact CDK activity provides insights into cell cycle regulation and potential cancer treatment strategies. -
HDAC1/2 and CDK2 Inhibitor
HDAC1/2 and CDK2-IN-1 is a dual inhibitor targeting HDAC1, HDAC2, and CDK2, with IC50 values of 70.7 μM, 23.1 μM, and 0.80 μM, respectively. This compound effectively disrupts the cell cycle and promotes apoptosis in tumor cells, demonstrating significant in vivo antitumor activity. It is suitable for research applications focused on cancer biology and therapeutic interventions targeting histone deacetylases and cyclin-dependent kinases.
