Catalog No.
Product Name
Application
Product Information
Citations
-
SKP2 Molecular Glue Degrader
XMU-MP-8 is a potent molecular glue degrader that targets the oncoprotein SKP2. It binds to the F-box domain of SKP2 and the N-terminal TPR domain of the E3 ligase STUB1, facilitating the formation of a stable SKP2-SKPer1-STUB1 ternary complex. This interaction leads to SKP2 ubiquitination and subsequent proteasomal degradation, selectively eliminating SKP2-expressing cancer cells. XMU-MP-8 demonstrates significant tumor suppression and favorable safety profiles in vivo, making it a valuable tool for cancer research, particularly in studies related to non-small cell lung adenocarcinoma (NSCLC) and prostatic adenocarcinoma. -
TRIM21 Molecular Glue
HGC652 is a molecular glue degrader that specifically targets TRIM21, facilitating the disruption of nuclear membrane integrity through a TRIM21-dependent mechanism. By binding with high affinity to the PRY-SPRY domain of TRIM21, HGC652 promotes the interaction between TRIM21 and NUP98, enhancing E3 ligase activity. This results in the polyubiquitination and subsequent proteasomal degradation of nucleoporins such as NUP155 and GLE1, leading to altered nuclear morphology, enhanced genomic instability, and ultimately, cancer cell death. HGC652 serves as a valuable tool for investigating nuclear envelope dynamics and the role of TRIM21 in cancer research. -
Molecular Glue
CC-647 is a molecular glue modulator that targets the Cereblon (CRBN) E3 ubiquitin ligase. It enhances the interaction between CRBN and ZBTB16, along with its oncogenic fusion protein RARĪ±-ZBTB16, with a DC50 of 103 nM. CC-647 is particularly valuable for the investigation of ZBTB16-RARĪ±-associated acute promyelocytic leukemia (APL) and offers potential insights into therapeutic strategies for this malignancy. -
Molecular Glues
MG Degrader 3 is a molecular glue that targets the CRBN protein, inducing targeted protein degradation. It exhibits potent anti-proliferative activity in multiple myeloma cell line MM.1S, with an IC50 of 8.7 nM. This compound is valuable for studies investigating protein degradation mechanisms and therapeutic approaches in cancer research. -
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. -
CDK2 Molecular Glue Degrader
CDK2 degrader 6 is a potent CDK2 molecular glue degrader that functions through binding to cereblon and CDK2, leading to the ubiquitination and proteasomal degradation of CDK2. With a DC50 of 46.5 nM, it effectively modulates the cell cycle and reduces proliferation in breast cancer cells. Additionally, CDK2 degrader 6 demonstrates in vivo antitumor activity in gastric cancer mouse models, making it a valuable tool for research into breast and gastric cancers. -
Molecular Glue Degrader
dCeMM3 is a molecular glue degrader that facilitates the ubiquitination and subsequent degradation of cyclin K. By promoting the interaction of the CDK12-cyclin K complex with the CRL4B ligase complex, dCeMM3 plays a critical role in regulating cell cycle progression. This reagent is particularly useful for research applications focused on targeted protein degradation and the elucidation of CDK12-associated pathways. -
Molecular Glue Degrader
dCeMM2 is a molecular glue degrader that specifically targets cyclin K. It induces ubiquitination and subsequent degradation of cyclin K by facilitating the interaction between CDK12-cyclin K and the CRL4B ligase complex. This compound is valuable for studying the regulation of cell cycle and transcriptional processes, and it serves as a tool in research areas focusing on cancer biology and cell signaling pathways. -
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. -
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. -
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. -
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. -
MYC Molecular Glues Degrader
MYC Degrader 1 is a potent molecular glue degrader that targets the MYC oncogene, facilitating the degradation of MYC proteins. This compound exhibits significant anti-tumor activity by restoring the functionality of the pRB1 protein, thereby reinstating the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors. MYC Degrader 1 is suitable for research applications focusing on cancer therapeutics and the modulation of MYC-driven signaling pathways. -
Molecule Glue
HuR degrader 2 is a molecular glue that specifically targets the RNA-binding protein Hu antigen R (HuR), leading to a significant degradation of approximately 30% of HuR at a concentration of 0.1 Ī¼M. This compound effectively inhibits the proliferation of the Colo-205 cancer cell line, demonstrating an IC50 of ā¤200 nM. Additionally, HuR degrader 2 shows a high affinity for cereblon, with an HTRF ratio of less than 0.02, making it a valuable tool for studying HuR's role in cancer biology. -
Molecular Glue
MG-HuR2 is a molecular glue degrader that specifically targets the oncogenic RNA-binding protein HuR, exhibiting an IC50 of 0.5 Ī¼M. This compound is particularly relevant for research involving HuR-overexpressing malignancies, such as breast cancer, providing a valuable tool for investigating therapeutic strategies aimed at modulating HuR activity in cancerous tissues. -
WEE1 Kinase Molecular Glue Degrader
BMS-986463 is a WEE1 kinase molecular glue degrader that functions as a CRBN E3 ligase modulator (CELMoD). It significantly inhibits tumor growth while reducing phospho-CDK2 levels, making it a valuable tool in cancer research. This compound is particularly relevant for studies focusing on advanced malignant solid tumors, including non-small cell lung cancer (NSCLC). -
Molecular Glue Degrader
WEE1 Degrader 1 is a CRBN-dependent molecular glue degrader that targets WEE1 and casein kinase 1Ī± (CK1Ī±) with sub-2 nM DC50 values for both proteins. This compound effectively induces the proteasomal degradation of its targets, providing a valuable tool for studying cell cycle regulation. WEE1 Degrader 1 is particularly relevant in the research of acute lymphoblastic leukemia, acute monocytic leukemia, acute promyelocytic leukemia, colorectal adenocarcinoma, and diffuse large B-cell lymphoma. -
SALL4/OSR1 Dual Molecular Glue Degrader
HRZ-01-082-5 is a dual-functional molecular glue degrader targeting SALL4 and OSR1, exhibiting a DC50 of 4.8 nM for OSR1. This compound effectively induces the degradation of both SALL4 and OSR1 via the CRBN mechanism. HRZ-01-082-5 is applicable in the study of heart and urogenital development as well as in cancer research, providing valuable insights into these critical biological processes. -
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-1Ī², IL-1Ī±, 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. -
STING Molecular Glue
NVS-STG2 is a molecular glue that targets the STING receptor by binding to the interstitial regions of adjacent STING dimers, thereby enhancing STING signaling. This compound promotes the activity of cGAMP, leading to the formation of larger and more stable oligomers, which amplifies the immune response. NVS-STG2 has demonstrated significant antitumor effects in preclinical animal models, making it a valuable tool for cancer immunotherapy research. -
IRF5/8 Molecular Glue Degrader
EN1033 is a covalent molecular glue degrader targeting immune regulatory transcription factors IRF5 and IRF8. It induces proteasome-dependent degradation of IRF5 and demonstrates a more rapid and robust degradation of IRF8. By covalently modifying specific residues, EN1033 destabilizes these factors, leading to a reduction in their pro-inflammatory transcriptional activity. This reagent is valuable for exploring mechanisms in autoimmune and inflammatory disorders. -
IKZF2 degrader
NVP-DKY709 is an orally active molecular glue degrader targeting IKZF2. This compound demonstrates a Dmax of 53% and a DC50 of 4 nM, indicating potent degradation efficacy. Additionally, NVP-DKY709 can also degrade IKZF4 and SALL4 with DC50 values of 13 nM and 2 nM, respectively. Its mechanism involves binding to CRBN, altering its conformation to facilitate the recruitment and degradation of IKZF2, thereby exerting significant anti-tumor activity. This functionality positions NVP-DKY709 as a valuable tool in cancer research and therapeutic development targeting IKZF protein family members. -
IKZF2 Molecular Glue Degrader
PLX-4545 is an orally active and selective molecular glue degrader that targets IKZF2 (zinc finger transcription factor Helios) via cereblon. This compound reprograms immunosuppressive regulatory T cells into pro-inflammatory effector T cells, thereby enhancing anti-tumor immune responses. PLX-4545 is intended for research applications related to solid tumors and the modulation of T cell functionality. -
IKZF2 Molecular Glue Degrader
(S,S)-PLX-4545 is a cereblon-based molecular glue degrader targeting IKZF2, a zinc finger transcription factor involved in immune regulation. This compound effectively promotes the degradation of IKZF2, making it a valuable tool for investigating IKZF2-related diseases, including various proliferative disorders and cancers. Researchers can leverage (S,S)-PLX-4545 to explore therapeutic strategies targeting IKZF2 functionality in different biological contexts. -
Enantiomer Of PLX-4545
(1S,2S,3R)-PLX-4545 is the (1S,2S,3R) enantiomer of PLX-4545, functioning as a selective cereblon-based molecular glue degrader that targets IKZF2 (zinc finger transcription factor Helios). This compound effectively reprograms immunosuppressive regulatory T cells into pro-inflammatory effector T cells, enhancing anti-tumor immune responses. Its applications extend to immunology and cancer research, providing insights into T cell modulation and potential therapeutic strategies for cancer immunotherapy. -
IKZF2 Selective and orally Inhibitor
PVTX-405 is a selective, orally bioavailable inhibitor targeting IKZF2, designed as a molecular glue degrader. With a DC50 of 0.7 nM and a Dmax of 91%, it enhances degradation efficiency while minimizing off-target effects, exhibiting an IC50 of 48 ĀµM for hERG inhibition. PVTX-405 demonstrates significant antitumor activity by inhibiting the growth of MC38 tumors and shows improved efficacy when combined with immune checkpoint therapies, such as anti-PD1 or anti-LAG3, in mouse models. -
Molecular Glue IKZF2-Degrader
IKZF2-degrader 3 is a molecular glue that selectively targets and degrades the IKZF2 protein, exhibiting a DC50 of 2.0 nM. It enhances the understanding of IKZF2's role in various biological processes and is useful for studying its implications in hematological malignancies. This reagent is valuable for research focused on targeted protein degradation and its therapeutic potential in cancer treatment. -
IKZF1 Degrader
IKZF1-degrader-2 is a molecular glue degrader that specifically targets IKZF1, facilitating its degradation in cancer cells. This compound exhibits potent anticancer activity while demonstrating low toxicity, making it a valuable tool for oncology research. IKZF1-degrader-2 is ideal for studies focused on targeted protein degradation and its therapeutic implications in cancer treatment. -
IKZF2 Degrader
IKZF2-degrader 2 is a selective molecular glue degrader that targets IKZF2, facilitating its ubiquitination and subsequent degradation through recruitment of the CRL4-CRBN E3 ubiquitin ligase. With DC50 values of 0.5 nM and 1.8 nM in HiBit and FACS assays, respectively, this compound also induces moderate degradation of SALL4 (DC50 of 9 nM) without significantly affecting IKZF1, IKZF3, CK1Ī±, or GSPT1. IKZF2-degrader 2 is suitable for investigating mechanisms in cancer immunology. -
IKZF2 Molecular Glue Degrader
IKZF2-degrader 1 is a selective IKZF2 molecular glue degrader that exhibits a DC50 of 0.5 nM, effectively targeting IKZF2 for degradation. With minimal activity against CK1Ī± (DC50: 210 nM), it provides a focused approach for studying the role of IKZF2 in cellular processes. This compound is valuable for researching IKZF2-dependent cancers, enabling investigations into its therapeutic potential and biological mechanisms. -
IKZF2 Degrader
IKZF2-degrader 4 is an IKZF2-targeting compound that facilitates the degradation of the IKZF2 protein. Through its mechanism, this degrader can disrupt the function of IKZF2, which is implicated in various cancer pathways. It is a valuable tool for investigating IKZF2's role in tumor biology and for exploring therapeutic strategies in cancer research. -
IKZF1 Degrader
IKZF1-degrader-1 is a molecular glue degrader targeting IKZF1, with a DC50 value of 0.134 nM. This compound facilitates the selective degradation of IKZF1, making it a valuable tool for research into tumor biology and potential cancer therapies. Its ability to modulate IKZF1 levels may provide insights into the role of this transcription factor in oncogenesis and therapeutic resistance. -
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. -
Immunomodulatory/Antineoplastic Agent
Lenalidomide hydrochloride is an oral immunomodulatory agent targeting cereblon (CRBN), acting as a molecular glue. It promotes the selective ubiquitination and degradation of transcription factors IKZF1 and IKZF3 via the CRBN-CRL4 ubiquitin ligase complex. This mechanism effectively inhibits the growth of mature B-cell lymphomas, including multiple myeloma, while also inducing the release of IL-2 from T cells, making it valuable in cancer research and therapeutic applications. -
Keap1-Cul3 E3 ligase Complex Allosteric Molecular Glues
VVD 065 is an allosteric modulator of the Keap1-Cul3 E3 ligase complex that functions as a molecular glue. By activating KEAP1, VVD 065 promotes the degradation of NRF2, an essential regulator of antioxidant defenses. This compound has demonstrated the ability to inhibit tumor growth in non-small cell lung cancer and esophageal squamous cell carcinoma xenograft models. VVD 065 serves as a valuable tool for research on cancer biology and therapeutic strategies targeting oxidative stress responses. -
Thrombin Inhibitor
PPACK dihydrochloride is a potent and selective irreversible inhibitor of thrombin. It serves as an alternative anticoagulant to lithium heparin for blood gas and electrolyte analyses in whole blood. Additionally, PPACK dihydrochloride inhibits plasminogen activator (rt-PA), preventing its binding to plasma protease inhibitors. This compound also reduces plasmin-induced endothelial permeability and morphological changes in bovine aortic endothelial cell monolayers, making it suitable for investigations in thrombosis-related research. -
Molecular Glue Degrader
(S)-dHTC1 is a molecular glue degrader that targets the transcriptional co-activator ENL. This compound exhibits high-affinity binding to the E3 ligase upon forming the ENL:dHTC1 complex, with an IC50 value of 93 nM. In MV4;11 cells, (S)-dHTC1 effectively degrades ENL, demonstrating a DC50 value of 26 nM. This reagent is valuable for studying mechanisms in acute myeloid leukemia. -
ALK Molecular Glue Degrader
TRI-611 is an orally active molecular glue degrader that targets the anaplastic lymphoma kinase (ALK). It forms a ternary complex with the substrate receptor CRBN, leading to polyubiquitination and subsequent degradation of ALK, including resistant fusion proteins. TRI-611 effectively inhibits ALK-mediated downstream signaling and exhibits anti-proliferative effects in ALK-positive cancer cells. Preclinical studies demonstrate its capability to induce regression of ALK-positive non-small cell lung cancer tumors, making it a valuable tool for research into TKI-refractory tumors and central nervous system metastases.
