Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
CDK2/CDK5 Inhibitor
(S)-PHA533533 is an inhibitor of cyclin-dependent kinases CDK2 and CDK5, demonstrating blood-brain barrier permeability with IC50 values of 37 nM and 55 nM, respectively. This compound effectively restores UBE3A expression by downregulating UBE3A-ATS, thereby alleviating the epigenetic silencing of paternal UBE3A in mature neurons. (S)-PHA533533 is a valuable tool for research applications related to Angelman syndrome and offers insights into therapeutic strategies for this genetic disorder. -
CDK9 Autophagic Degrader
CDK9 autophagic degrader 1 is a selective autophagic degrader targeting cyclin-dependent kinase 9 (CDK9). This compound effectively degrades CDK9, leading to a significant reduction in associated Cyclin T1 levels. Demonstrating over 80% inhibition of CDK9 at a concentration of 100 nM, this reagent serves as a valuable tool for research applications focused on transcriptional regulation and cancer biology. -
CDK2 Inhibitor
CDK2-IN-12 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 11.6 μM. This compound also inhibits human carbonic anhydrase isoforms I, II, IX, and XII, with respective KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 demonstrates notable anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development. -
CA/CDK2 Inhibitor
Carbonic anhydrase inhibitor 14 is a potent inhibitor of carbonic anhydrases (CAs), exhibiting Ki values of 1203 nM for hCA I, 99.7 nM for hCA II, 9.4 nM for hCA IX, and 27.7 nM for hCA XII. Additionally, it effectively inhibits cyclin-dependent kinase 2 (CDK2) with an IC50 of 20.3 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications targeting both CA and CDK2 pathways. -
CDK2 Inhibitor
CDK2-IN-11 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), demonstrating an IC50 of 6.4 μM. With inhibitory constant (KI) values of 23.4 nM, 56.3 nM, and 44.3 nM for human carbonic anhydrases II, IX, and XII, respectively, it exhibits significant enzyme inhibition. CDK2-IN-11 is primarily utilized in anticancer research, making it a valuable tool for studies targeting cell cycle regulation and tumor progression. -
CDK/GSK3β/JNK Inhibitor
Indirubin-3′-oxime (IDR3O) is a synthetic derivative of indirubin that functions as a potent inhibitor of cyclin-dependent kinases (CDKs), glycogen synthase kinase 3β (GSK3β), and all three isoforms of c-Jun N-terminal kinases (JNK1, JNK2, JNK3). It demonstrates inhibitory activity with IC50 values of 0.8 μM, 1.4 μM, and 1.0 μM for each JNK isoform, respectively. Indirubin-3′-oxime is also known to promote chondrocyte height growth through the activation of Wnt/β-catenin signaling, making it relevant for studies in cellular growth and differentiation. -
CDK4/6 Inhibitor
Palbociclib hydrochloride is a selective inhibitor of cyclin-dependent kinases CDK4 and CDK6, with IC50 values of 11 nM and 16 nM, respectively. This compound demonstrates significant anti-proliferative activity, effectively inducing cell cycle arrest in malignant cells. Palbociclib hydrochloride is utilized in research focused on HR-positive and HER2-negative breast cancer as well as hepatocellular carcinoma, making it a valuable tool for understanding tumor biology and therapeutic responses. -
CDK7 Inhibitor
YKL-5-124 is a selective and irreversible inhibitor of cyclin-dependent kinase 7 (CDK7), demonstrating IC50 values of 53.5 nM and 9.7 nM for CDK7 and the CDK7/Mat1/CycH complex, respectively. This compound exhibits over 100-fold selectivity for CDK7 compared to CDK9 and CDK2 and has negligible activity against CDK12 and CDK13. YKL-5-124 effectively induces cell-cycle arrest, inhibits E2F-driven transcription, and has a limited impact on the phosphorylation status of RNA polymerase II, making it a valuable tool for research in cell cycle regulation and transcriptional control. -
CDK Inhibitor
Romaciclib monohydrochloride is a selective CDK inhibitor that targets CDK8 and CDK19. This compound exhibits potent inhibition of CDK8/CycC and CDK19/CycC kinase activities with IC50 values of 4.4 nM and 10.4 nM, respectively. Additionally, it weakly inhibits CDK9 with an IC50 of 1070 nM, while having no significant activity against other CDK isoforms. Romaciclib monohydrochloride is known to inhibit the phosphorylation of STAT1 at S727 and STAT5 at S726, demonstrating potential anti-tumor activity valuable for cancer research applications. -
CDK9 Inhibitor
KB-0742 dihydrochloride is a selective and orally bioactive inhibitor of CDK9, exhibiting an IC50 of 6 nM for the CDK9/cyclin T1 complex. This compound demonstrates over 50-fold selectivity for CDK9 compared to other CDK kinases, making it a valuable tool for precision research. KB-0742 dihydrochloride possesses strong anti-tumor activity, facilitating investigations into its efficacy in cancer biology and therapeutic applications. -
CDK4/6 Inhibitor
Dalpiciclib is a highly selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), demonstrating IC50 values of 12.4 nM and 9.9 nM, respectively. This orally active compound exhibits significant antitumor activity, particularly in breast cancer and esophageal squamous cell carcinoma. Dalpiciclib is utilized in research applications focused on tumor suppression and cell cycle regulation. -
Cyclin K Degrader
HQ461 is a molecular glue that facilitates the interaction between CDK12 and DDB1, leading to the targeted degradation of cyclin K. This degradation impairs CDK12 function, which in turn results in reduced phosphorylation of CDK12 substrates, downregulation of DNA damage response genes, and induces apoptosis in affected cells. HQ461 is a valuable tool for research applications focused on the modulation of cell cycle regulation and the DNA damage response pathway. -
CDK9 Inhibitor
KB-0742 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), exhibiting an IC50 of 6 nM for the CDK9/cyclin T1 complex. With over 50-fold selectivity against other CDK kinases, KB-0742 demonstrates significant anti-tumor activity. This compound is particularly valuable for research involving transcriptional regulation, cancer biology, and therapeutic strategies targeting CDK9-associated pathways. -
CDK4/6 Inhibitor
Dalpiciclib hydrochloride is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), with IC50 values of 12.4 nM and 9.9 nM, respectively. This compound exhibits significant antitumor activity, particularly in the context of breast cancer and esophageal squamous cell carcinoma. Dalpiciclib hydrochloride is valuable for research focused on cell cycle regulation and cancer therapeutics. -
PTEFb/CDK9 Inhibitor
Atuveciclib is a highly selective oral inhibitor of PTEFb/CDK9, demonstrating potent activity with an IC50 of 13 nM against the CDK9/CycT1 complex. This compound effectively disrupts transcriptional regulation, making it a valuable tool in cancer research and studies related to transcriptional control. Atuveciclib may be employed in investigations aimed at understanding the roles of CDK9 in various diseases, including cancer and other pathologies linked to aberrant transcriptional activity. -
CDK5 Inhibitor
GFB-12811 is a highly selective inhibitor of cyclin-dependent kinase 5 (CDK5) with an IC50 of 2.3 nM. Its potent action allows for effective modulation of CDK5 activity, making it a valuable tool for studying neurodegenerative diseases and related signaling pathways. This compound is suitable for research investigating the role of CDK5 in neuronal function and pathology. -
CDK4/6 Inhibitor
Abemaciclib metabolite M20 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). This compound exhibits potent anti-proliferative activity in various cancer cell lines, contributing to its potential use in cancer therapy. Research applications include studying cell cycle regulation and exploring therapeutic strategies for tumors driven by CDK4/6 activity. -
CDK2/5 Inhibitor
CDK5 inhibitor 20-223 is a potent inhibitor of cyclin-dependent kinases 2 and 5, exhibiting IC50 values of 6.0 nM and 8.8 nM, respectively. This compound demonstrates significant anti-colorectal cancer activity, making it a valuable tool for research in cancer biology and therapeutic development. Its selective inhibition of CDK2 and CDK5 provides insights into their roles in cell cycle regulation and oncogenesis. -
CCND1/CDK4 PROTAC Degrader
CPD-39 is a potent heterobifunctional PROTAC degrader that targets CCND1 and CDK4. This compound effectively induces the degradation of these proteins, demonstrating significant anti-proliferative activity. CPD-39 is intended for research applications focusing on the modulation of cell cycle regulation and cancer therapeutics. -
CDK4/6 Inhibitor
Abemaciclib metabolite M18 hydrochloride functions as a CDK4/6 inhibitor, exhibiting significant antitumor activity. This compound has been utilized in the design of PROTAC (Proteolysis Targeting Chimera) CDK4/6 degraders in conjunction with a CRBN ligand. Its role in targeted protein degradation research makes it a valuable tool for investigating cell cycle regulation and cancer therapeutics. -
CDK12 Inhibitor
CDK12-IN-2 is a selective inhibitor of cyclin-dependent kinase 12 (CDK12), exhibiting a nanomolar potency with an IC50 value of 52 nM. This compound also demonstrates inhibitory activity against CDK13, its closest homologue, but maintains strong selectivity for CDK12 over other kinases such as CDK2, CDK7, CDK8, and CDK9. CDK12-IN-2 effectively inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II, making it a valuable chemical probe for functional studies in cancer biology and transcription regulation. -
CDK5 Inhibitor
CDK5-IN-3 is a highly selective inhibitor of CDK5, demonstrating IC50 values of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. This compound is valuable for investigations into the role of CDK5 in cellular processes and is particularly relevant for research focused on autosomal dominant polycystic kidney disease (ADPKD). Its potency and specificity make CDK5-IN-3 an essential tool for elucidating the molecular mechanisms underlying CDK5-related pathologies.
