Catalog No.
Product Name
Application
Product Information
Citations
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CDK2/CDK5 PROTAC Degrader
TMX-2172 is a selective bivalent PROTAC that targets CDK2 and CDK5, inducing their proteasomal degradation with IC50 values of 6.5 nM and 6.8 nM, respectively. This compound demonstrates notable selectivity for CDK2 and CDK5, while sparing other cyclin-dependent kinases such as CDK1, CDK4, CDK6, CDK7, and CDK9. TMX-2172 effectively inhibits the enzymatic activity of CDK2 and CDK5, leading to a reduction in ASCL1 protein levels, induction of cancer cell death, and antiproliferative effects. This reagent is applicable in research focused on ovarian cancer and small cell lung cancer. -
CDK12/7/9 Degrader
BSJ-5-63 is a potent PROTAC degrader targeting CDK12, CDK7, and CDK9. It effectively reduces protein expression levels of these kinases as well as RNAPII and Cyclin K, resulting in decreased mRNA expression of BRCA1 and BRCA2. This compound exhibits significant anticancer activity and is particularly relevant for research focused on prostate cancer. -
CDK12/CDK13 PROTAC Degrader
ZLC491 is a PROTAC degrader that selectively targets CDK12 and CDK13, utilizing cereblon- and proteasome-dependent mechanisms for degradation. This compound effectively inhibits the transcription and expression of long genes, particularly those involved in DNA damage response pathways. ZLC491 demonstrates anti-proliferative effects in various triple-negative breast cancer cell lines, making it a valuable tool for research into targeted therapies for this aggressive cancer subtype. -
PROTAC/CDK2 Degrader
CDK2 Degrader 2 is a potent PROTAC targeting cyclin-dependent kinase 2 (CDK2), facilitating its degradation in MKN1 cells with a DC50 value of less than 100 nM. This compound employs a novel design, integrating a ligand for the target protein along with a linker and a ligand for the E3 ligase cereblon (CRBN). CDK2 Degrader 2 is valuable for research applications focused on the regulation of cell cycle progression and the exploration of targeted protein degradation mechanisms. -
Molecular Glue Degrader
dCeMM4 is a molecular glue degrader that targets cyclin K by inducing its ubiquitination and subsequent degradation. It facilitates the interaction between CDK12-cyclin K and the CRL4B ligase complex, leading to effective protein degradation. This compound is useful for research applications investigating cell cycle regulation and the ubiquitin-proteasome system. -
PROTAC CDK9 Degrader
PROTAC CDK9 degrader-9 is a selective and potent degrader designed to target cyclin-dependent kinase 9 (CDK9) via PROTAC technology. This compound facilitates the targeted degradation of CDK9, thereby modulating transcriptional regulation and influencing cell proliferation. It is particularly useful in anti-cancer research, where the inhibition of CDK9 can lead to suppression of oncogenic pathways. -
PROTAC CDK9 degrader
PROTAC CDK9 degrader-2, a selective degrader of cyclin-dependent kinase 9 (CDK9), utilizes a PROTAC mechanism involving a natural product ligand, Wogonin, which targets the ubiquitin E3 ligase Cereblon (CRBN). With an IC50 of 17 μM in MCF-7 cell lines, this compound demonstrates potent activity in the degradation of CDK9, making it a valuable reagent for research applications focused on CDK9-related pathways in cancer biology and therapeutic development. -
CDK2 Degrader
(R)-CDK2 Degrader 6 is a cereblon-based molecular glue degrader specifically targeting cyclin-dependent kinase 2 (CDK2). It functions by inducing ubiquitination and subsequent proteasomal degradation of CDK2, with a DC50 value of 27 nM. This compound is suitable for cancer research applications, providing a valuable tool for studying CDK2-related pathways and therapeutic interventions. -
CDK2 Molecular Glue Degrader
(S)-CDK2 degrader 6 selectively targets cyclin-dependent kinase 2 (CDK2) as a molecular glue degrader. With a DC50 of 166.7 nM over 24 hours, this compound effectively promotes the degradation of CDK2, thereby modulating cell cycle progression. It holds significant potential for applications in breast cancer research, enabling the exploration of therapeutic strategies that involve the regulation of CDK2 activity. -
Ligands for Target Protein for PROTAC
FN-1501-propionic acid is a ligand targeting cyclin-dependent kinases 2 and 9 (CDK2/9), utilized in the development of PROTAC (proteolysis targeting chimeras) for targeted protein degradation. This compound can be combined with a CRBN ligand to facilitate the design of PROTAC-based CDK2/9 degraders, enabling selective degradation of these kinases. Its application in research enhances the study of cellular processes regulated by CDK2 and CDK9, making it a valuable tool for investigating therapeutic strategies against diseases associated with dysregulated kinase activity. -
CDK9 PROTAC Degrader
PROTAC CDK9 degrader-11 is an orally active PROTAC degrader that specifically targets CDK9, demonstrating a DC50 value of 1.09 nM. This compound shows cytotoxicity in various small cell lung cancer cell lines with an IC50 in the nanomolar range. PROTAC CDK9 degrader-11 effectively induces cell cycle arrest at the G0/G1 phase and reduces invasion in DMS114 and DMS53 cells. Additionally, it exhibits significant antitumor efficacy in NCI-H446 xenograft mouse models, making it a valuable tool for cancer research and therapeutic development. -
CDK4/6 PROTAC Degrader
CST651 is a selective proteolysis-targeting chimera (PROTAC) degrader specifically designed to target cyclin-dependent kinases CDK4 and CDK6. This compound effectively degrades CDK4 and CDK6 in MM.1S cells, exhibiting DC50 values of 20 nM and 5.1 nM, respectively. CST651 demonstrates the ability to inhibit cancer cell proliferation and migration, making it a valuable tool for research into various cancers, including acute lymphoblastic leukemia. -
PROTAC Degrader
PROTAC CDK2 Degrader-1 is a selective PROTAC degrader designed to target cyclin-dependent kinase 2 (CDK2). This compound effectively induces degradation of CDK2 and inhibits phosphorylation of the retinoblastoma (RB) protein in the CDK2-dependent OVCAR3 cell line, with an IC50 range of 100-500 nM. It serves as a valuable tool for investigating the biological functions of CDK2 in cancer research and therapeutic applications. -
Molecular Glues
CDK12 ligand-3 is a molecular glue that effectively targets and degrades the CDK12 protein, with a DC50 of 35 nM. This compound also influences the degradation of CDK13 and its regulatory partner, Cyclin K, while inhibiting serine 2 phosphorylation of the RNA polymerase II CTD. CDK12 ligand-3 demonstrates significant anti-proliferative effects on Jurkat cells and is applicable in cancer research, particularly in the study of leukemia. -
CDK9 Degrader
PROTAC CDK9 degrader-8 is a potent degrader targeting CDK9, exhibiting an IC50 value of 0.01 μM. This compound effectively induces the degradation of CDK9, making it a valuable tool for investigating the role of CDK9 in cancer biology and therapeutic resistance. It is suitable for use in studies aimed at understanding the mechanisms of tumor progression and exploring potential treatment strategies. -
CDK12/CDK13 Inhibitor/CycK Molecular Glue Degrader
SR-5037 is an orally active inhibitor of CDK12 and CDK13, with an IC50 of 31 nM, and functions as a molecular glue degrader for CycK, demonstrating a DC50 of 30 nM and Dmax exceeding 98%. By inhibiting the enzymatic activity of the CDK12/CycK and CDK13/CycK complexes, SR-5037 facilitates the recruitment of DDB1, leading to proteasome-mediated degradation of CycK. This compound has shown efficacy in degrading active CycK in mouse models of triple-negative breast cancer and is a valuable tool for investigating treatment options in such malignancies. -
CDK2/4/6 PROTAC Degrader
PROTAC CDK2/4/6 Degrader-1 is a potent orally bioavailable degrader targeting CDK2, CDK4, and CDK6 through the proteolysis-targeting chimera (PROTAC) mechanism. This compound functions by facilitating the ubiquitination and degradation of these cyclin-dependent kinases, thereby inhibiting their activity. Its applications extend to the study of malignant melanoma, providing valuable insights into tumor biology and potential therapeutic interventions. This degrader is synthesized as a prodrug from PROTAC CDK2/4/6 Degrader-2, enabling enhanced functionality in biological systems. -
CDKs PROTAC Degrader
TMX-2138 is a potent CDKs PROTAC degrader that achieves IC50 values of 8.7 nM for CDK1/cyclinB, 10.9 nM for CDK2/cyclinA, 7.0 nM for CDK5/p25, and 25.7 nM for CDK9/cyclinT1. This compound facilitates the ubiquitination and subsequent degradation of cyclin-dependent kinases (CDKs), making it a valuable tool for investigating their roles in cellular processes. TMX-2138 is particularly relevant for research focused on ovarian cancer, enabling the study of CDK-targeted therapies and their potential therapeutic implications. -
CDK9 Degrader/Ligands for Target Protein for PROTAC
(R)-PROTAC CDK9 ligand-1 is a potent degrader targeting cyclin-dependent kinase 9 (CDK9), a key regulator of transcription and cell cycle progression. This compound facilitates the synthesis of PROTACs (proteolysis-targeting chimeras), which exhibit antitumor activity by promoting the degradation of CDK9. Research applications include investigations into cancer biology and therapeutic strategies aimed at modulating CDK9 levels for improved treatment outcomes. -
PROTAC USP7 Degrader
PROTAC USP7 Degrader-2 targets the ubiquitin-specific protease 7 (USP7) and functions as a selective degrader. Demonstrating a DC50 of 1.91 μM in TE-12 cells, this compound effectively inhibits the migration of upper gastrointestinal tract cancer cells, although its anti-proliferative activity is relatively modest. PROTAC USP7 Degrader-2 is valuable for research focused on metastatic upper gastrointestinal cancer, aiding in the exploration of therapeutic strategies targeting USP7. -
MNK1 PROTAC Degrader
PROTAC MNK1 degrader-1 is a selective degrader that targets MNK1, exhibiting a DC50 of 11.92 nM and a Dmax exceeding 96% in MV4-11 cells. This compound effectively reduces phosphorylated eIF4E levels (IC50: 22.07 nM), triggers apoptosis, and causes G1 phase cell cycle arrest. With demonstrated potent antitumor activity, PROTAC MNK1 degrader-1 also shows robust antileukemic efficacy in MV4-11 xenograft mouse models while maintaining acceptable drug safety profiles. -
SARS-CoV-2 Mpro PROTAC degrader
HP211206 is a PROTAC degrader targeting the main protease (Mpro) of SARS-CoV-2, designed to selectively degrade both the protease and its drug-resistant variants. This compound demonstrates an IC50 of 181.9 nM and a DC50 of 621 nM, reflecting its potency in disrupting viral replication. HP211206 also exhibits antiviral activity, making it a valuable tool for research aimed at understanding and combating SARS-CoV-2 infections. -
SARS-CoV-2 Mpro PROTAC Degrader
PROTAC SARS-CoV-2 Mpro degrader-2 is a highly effective PROTAC degrader targeting the main protease (Mpro) of SARS-CoV-2. This compound exhibits significant antiviral activity against various coronaviruses, including EC50 values of 10.8 μM for SARS-CoV-2, 1.6 μM for HCoV-OC43, and 6.5 μM for HCoV-229E. In Calu-3 cells, it demonstrates potent efficacy with an EC50 of 0.89 μM, making it a valuable tool for research focused on coronavirus biology and potential therapeutic interventions. -
NEK7 Molecular Glue Degrader
NEK7 degrader-3 is an orally active NEK7 molecular glue degrader with a DC50 of 33.1 nM, which effectively mediates the interaction between NEK7 and the E3 ligase cereblon, leading to the proteasomal degradation of NEK7. This degradation process attenuates NLRP3 inflammasome-mediated inflammatory responses, resulting in the inhibition of caspase-1 activity and the release of pro-inflammatory cytokines IL-1β, IL-1α, and IL-18. NEK7 degrader-3 demonstrates significant anti-inflammatory effects in LPS-induced neuroinflammation mouse models, serving as a valuable tool for research focused on neuroinflammation. -
Molecular Glue
ABT-002 is a molecular glue degrader that targets GSPT1 and NEK7, enhancing the ubiquitin-proteasome system's ability to degrade these proteins. This compound is the active metabolite of ABS-752 and demonstrates potential in the research of hepatocellular carcinoma (HCC). Its unique mechanism of action makes it a valuable tool for elucidating cellular pathways and therapeutic strategies in cancer biology. -
GSPT1/NEK7 Degrader
ABS-752 is a potent molecular glue degrader targeting GSPT1 and NEK7. It demonstrates significant cytotoxicity by reducing the protein levels of both GSPT1 and SALL4, along with NEK7. As a prodrug, ABS-752 is activated by monoamine oxidase, VAP-1, into an aldehyde intermediate and further converted to its active form, ABT-002. This compound has promising applications for research into hepatocellular carcinoma. -
GSPT1 Molecular Glue
ABS-752 hydrochloride is a prodrug that targets GSPT1 through CRBN modulation, functioning as a molecular glue. It effectively degrades GSPT1 and NEK7, without forming ternary complexes with CRBN and neosubstrates. The compound is activated by the enzyme VAP-1, converting it into an aldehyde intermediate and subsequently yielding the active molecule, ABT-002. ABS-752 is utilized in research focused on hepatocellular carcinoma (HCC) and related therapeutic pathways. -
H-PGDS PROTAC Degrader
PROTAC(H-PGDS)-7 is a targeted protein degradation agent that selectively degrades hematopoietic prostaglandin D synthase (H-PGDS). With a DC50 value of 17.3 pM, it demonstrates potent biological activity in modulating the levels of H-PGDS. This compound is valuable for research applications involving the role of H-PGDS in inflammatory processes and may assist in elucidating therapeutic strategies for related diseases. -
H-PGD PROTAC Degrader
PROTAC(H-PGDS)-8 is a targeted protein degradation compound that specifically degrades hematopoietic prostaglandin D synthase (H-PGDS) with an IC50 of 0.14 μM. This PROTAC molecule facilitates the ubiquitination and subsequent proteasomal degradation of H-PGDS, making it a valuable tool for investigating the role of H-PGDS in various biological processes. Research applications include studies on inflammation, pain mechanisms, and other pathophysiological conditions where H-PGDS is implicated. -
PROTAC Degrader
RP03707 is a potent PROTAC degrader targeting KRASG12D. By forming a ternary complex with KRASG12D and the CRBN E3 ligase, RP03707 facilitates the ubiquitination and subsequent proteasomal degradation of KRASG12D. This compound demonstrates significant inhibitory effects on the growth of KRASG12D-positive tumor cells, making it an essential tool for research in cancer biology and targeted therapy development. -
K-Ras PROTAC Degrader
PROTAC K-Ras Degrader-3 is a powerful PROTAC compound designed to target and degrade K-Ras, demonstrating a DC50 of ≤ 1 nM in SW620 KRAS G12D cells and a GI50 of ≤ 10 nM for inhibiting SW620 3D cell growth. This compound is particularly valuable in cancer research, especially for studying non-small-cell lung cancer (NSCLC). Its unique design incorporates a K-RAS ligand, a Cereblon ligand, and a linker, facilitating targeted degradation and offering insights into K-Ras-related pathways. -
Molecular Glues
PRLX-93936 is a molecular glue that targets the TRIM21 ubiquitin ligase to facilitate the degradation of nuclear pore complexes. By binding to TRIM21 and forming a ternary complex with TRIM21 and NUP98, this compound mediates ubiquitination and proteasomal degradation of NUP98 and related proteins. PRLX-93936 induces apoptosis in cancer cells, reduces the levels of short-lived cytoplasmic mRNA transcripts, and inhibits the activated Ras signaling pathway. It demonstrates significant antitumor activity in mouse models, particularly for pancreatic cancer and multiple myeloma, making it a valuable tool for cancer research. -
KRAS G12D Molecular Glue Degrader
IPS-06061 is a molecular glue degrader that targets the KRAS G12D mutant through the formation of a ternary complex with CRBN. This compound effectively degrades KRAS G12D with a DC50 value of less than 500 nM, demonstrating significant anti-tumor efficacy. It serves as a valuable tool for research into targeted therapies for cancers driven by KRAS mutations. -
KRAS(on) PROTAC Degrader
ACBI-4 is a selective PROTAC degrader targeting the active state of KRAS (KRAS(on)). This compound exhibits significant anti-proliferative effects and effectively degrades various KRAS mutants, including KRASG12R, in cancer cell models. ACBI-4 is valuable for research applications focused on understanding KRAS-mediated signaling pathways and developing targeted cancer therapies. -
Pan-KRAS PROTAC Degrader
PROTAC pan-KRAS degrader-1 targets pan-KRAS mutations, facilitating the degradation of various KRAS variants, including G12D, G12C, G12V, and G13D. This compound exhibits potent activity against the G12D mutation in AGS cells, achieving a DC50 of 1.1 nM and a maximum degradation efficacy (Dmax) of 95%. PROTAC pan-KRAS degrader-1 is a valuable tool for investigating diseases associated with KRAS mutations and amplifications, particularly in cancer types such as breast, bladder, and gastric cancer. -
p300/CBP Degrader
MJP6412 is a selective degrader of the histone acetyltransferases p300 and CBP, exhibiting DC50 values of 1.6 nM and 1.2 nM, respectively. This compound effectively induces degradation of these proteins, thereby modulating acetylation levels in cells. MJP6412 is particularly relevant in cancer research, providing insights into the role of p300 and CBP in oncogenic processes and potential therapeutic interventions. -
PROTAC KDM5B Degrader
GT-653 is a PROTAC degrader targeting lysine-specific demethylase 5B (KDM5B). It efficiently induces degradation of KDM5B by 68.35% at a concentration of 10 μM through a ubiquitin proteasome-dependent mechanism. This compound elevates H3K4me3 levels and activates type-I interferon signaling pathways in prostate cancer cells, specifically in the 22RV1 cell line. Research applications include studying KDM5B's role in cancer biology and evaluating potential therapeutic strategies that involve epigenetic modulation. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-12 is a CRBN-recruiting PROTAC designed to selectively degrade the EZH2 protein, exhibiting an IC50 of 3.90 nM for EZH2 and an IC50 of 5.24 μM for EZH1. This compound facilitates targeted protein degradation, making it a valuable tool for research focused on epigenetic regulation and cancer biology. Its ability to modulate the expression of key oncogenic factors positions it as a significant reagent for therapeutic investigations targeting EZH2-dependent pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-24 is an innovative molecule designed to target EZH2 by utilizing a PROTAC-mediated degradation mechanism. This compound exhibits potent EZH2 methyltransferase inhibitory activity, facilitating the selective degradation of the EZH2 protein. Research applications include studies on epigenetic regulation and therapeutic strategies for cancers with aberrant EZH2 activity. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-30 is a PROTAC protein degrader specifically designed to target the enhancer of zeste homolog 2 (EZH2) with an IC50 of 6.22 μM in SU-DHL-6 cells. This compound is instrumental in research applications focusing on diffuse large B-cell lymphoma by promoting the degradation of EZH2 and thereby modulating epigenetic regulation. The inclusion of ligands for both EZH2 and MDM2, coupled with a linker, facilitates targeted protein degradation and offers a valuable tool for investigating therapeutic strategies in cancer biology. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-43 is a targeted PROTAC protein degrader that specifically degrades the EZH2 protein, exhibiting an IC50 of 21.73 μM in SU-DHL-6 cells. This compound is valuable for investigating the role of EZH2 in lymphoma research and understanding its mechanistic function in histone methylation. The dual ligand design incorporates a histone methyltransferase ligand and a VHL ligand, promoting efficient substrate recognition and recruitment for proteasomal degradation. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-17 is a selective protein degrader that targets the enhancer of zeste homolog 2 (EZH2). This compound demonstrates significant antiproliferative activity, with an IC50 of 18.32 μM in lymphoma cell lines. PROTAC EZH2 Degrader-17 is a valuable tool for investigating EZH2-related pathologies and provides insights into the therapeutic potential of protein degradation in cancer research. -
EZH2 Ligand
EZH2 ligand-3 functions as a ligand targeting the Enhancer of Zeste Homolog 2 (EZH2) protein. This compound plays a crucial role in the synthesis of PROTAC EZH2 Degrader-35, facilitating the selective degradation of EZH2 in cellular models. It is valuable for research applications focused on epigenetic regulation and targeted protein degradation strategies. -
EZH2 PROTAC
PROTAC EZH2 Degrader-26 is a targeted proteolysis-targeting chimera (PROTAC) designed to specifically degradation of the enhancer of zeste homolog 2 (EZH2). This compound demonstrates a potent inhibitory activity with an IC50 of 5.80 nM against EZH2, alongside micromolar-level activity against EZH1, with an IC50 of 0.06 μM. PROTAC EZH2 Degrader-26 is suitable for research applications involving epigenetic regulation, cancer biology, and studies aimed at understanding histone methylation processes. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-39 is a targeted PROTAC that effectively degrades the EZH2 protein, exhibiting an IC50 of 61.00 nM. This compound functionally inhibits the methyltransferase activity of EZH2, making it an important tool for studying the biological implications of EZH2 modulation. Its applications include cancer research and epigenetic regulation studies, contributing to advancements in targeted therapy development. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-15 is a targeted degrader that specifically interacts with the EZH2 protein via a proteolysis-targeting chimera (PROTAC) mechanism. This compound effectively inhibits the methyltransferase activity of EZH2, leading to its degradation and resulting in alterations to histone methylation patterns. It serves as a valuable tool for research applications focused on epigenetic regulation, cancer biology, and therapeutic strategies aimed at EZH2 modulated pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-10 is a Proteolysis Targeting Chimeras (PROTAC) compound designed to selectively degrade the enhancer of zeste homolog 2 (EZH2). By facilitating the ubiquitination and subsequent proteasomal degradation of EZH2, this compound exhibits potential as an innovative therapeutic approach for cancer research. Its mechanism involves a specific ligand for EZH2 and a cereblon ligand, linked together to enhance degradation efficiency, making it a valuable tool for investigating EZH2-related oncogenic pathways. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-35 is a proteolysis-targeting chimera (PROTAC) specifically designed to degrade the Enhancer of Zeste Homolog 2 (EZH2) protein, exhibiting a binding affinity (Ka) of 16.19 nM. This compound demonstrates significant antiproliferative activity against triple-negative breast cancer cells while maintaining minimal cytotoxicity toward normal human epithelial, hepatic, and renal cells. PROTAC EZH2 Degrader-35 is a valuable tool for studying the role of EZH2 in cancer biology and has potential applications in therapeutic research focused on triple-negative breast cancer. -
EZH2 PROTAC
PROTAC EZH2 Degrader-27 is a potent EZH2 PROTAC inhibitor with an IC50 of 4.00 nM, specifically designed to target the SET domain of the EZH2 methyltransferase. By engaging in targeted protein degradation, this compound effectively inhibits methyltransferase activity, leading to downregulation of histone methylation. Research applications include studies on epigenetic regulation and potential therapeutic strategies targeting EZH2 in various cancers. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-13 is a targeted proteolysis-targeting chimera (PROTAC) designed to selectively degrade Enhancer of Zeste Homolog 2 (EZH2) with an IC50 of 2.70 nM. This compound exhibits potent antiproliferative effects in various cancer cell lines, making it a valuable tool in cancer research. PROTAC EZH2 Degrader-13 facilitates investigations into the role of EZH2 in tumorigenesis and therapeutic resistance, providing insights for the development of innovative cancer treatments.
