Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
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. -
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. -
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 µM 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, CK1α, 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 CK1α (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. -
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. -
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. -
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. -
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. -
Cereblon E3 Ubiquitin Ligase Modulating Agent
CC-92480 is a cereblon E3 ubiquitin ligase modulating drug (CELMoD). CC-92480 shows high affinity to cereblon, resulting in potent antimyeloma activity. -
Molecular Glue
(R)-CR8 trihydrochloride is a potent inhibitor of CDK1, CDK2, CDK5, CDK7, and CDK9, functioning as a molecular glue degrader that targets cyclin K. With inhibitory activity characterized by low nanomolar IC50 values, it effectively induces apoptosis while exhibiting neuroprotective properties. This compound is suitable for research applications in cancer biology and neurodegenerative disease studies. -
Molecular Glues
(S)-Thalidomide is the S-enantiomer of Thalidomide, functioning as a molecular glue. It exerts significant biological activities, including immunomodulation, anti-inflammation, antiangiogenesis, and pro-apoptosis. This compound induces teratogenic effects through its interaction with cereblon (CRBN), making it a valuable tool for research into cell signaling pathways and developmental biology. -
CDK12/CCNK Molecular Glue
NCT02 is a molecular glue degrader that targets CDK12 through the E3 ubiquitin ligase DDB1, resulting in the ubiquitination and subsequent proteasomal degradation of its partner protein CCNK. This mechanism leads to the downregulation of CDK12, inhibiting its downstream signaling pathways. NCT02 exhibits significant biological activity by inducing apoptosis in tumor cells, arresting the cell cycle, and selectively inhibiting the proliferation of colorectal cancer cells with TP53 mutations or belonging to the CMS4 molecular subtype. Additionally, NCT02 demonstrates potential in suppressing tumor growth in both in vitro and in vivo models. -
Molecular Glue Degrader
VNPP433-3β is an orally active molecular glue degrader that targets androgen receptor (AR) and its splice variants (AR-Vs), as well as MAP kinase-interacting serine/threonine protein kinases Mnk1/2. This compound induces apoptosis in cells and demonstrates significant inhibition of tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β is a valuable tool for investigating mechanisms in castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
CCNK Molecular Glue Degrader
ZLY025 is a potent CCNK molecular glue degrader with a DC50 of 42.7 nM. This compound demonstrates significant antiproliferative effects across a range of tumor cell lines, exhibiting IC50 values between 0.08 and 2.45 μM. ZLY025 is capable of inducing apoptosis and causing G1 phase cell cycle arrest, making it a valuable tool for cancer research, particularly in the study of lung cancer. -
IKZF2/CK1α Molecule Glue
DEG-35 is a CRBN-dependent dual degrader targeting IKZF2 and CK1α, exhibiting DC50 values of 1.4 nM and 4.4 nM, respectively. This compound activates the p53 apoptosis pathway, highlighting its potential in promoting cell death. DEG-35 serves as a valuable tool for research focused on Acute Myeloid Leukemia (AML), providing insights into targeted degradation strategies for therapeutic applications. -
CK1α molecular glue
dCK1α-2 is an orally active CK1α molecular glue degrader that targets proteins involved in the p53 signaling pathway. This compound demonstrates significant anti-tumor efficacy in preclinical mouse models and promotes the expression of p53-related genes, making it a valuable tool for research on cancer biology and therapeutic interventions aimed at restoring p53 function. Its mechanism of action provides insights into targeted degradation strategies in cancer treatment. -
CK1α Molecular Glue Degrader
QXG-6442 is a CK1α molecular glue degrader that effectively targets and degrades CK1α with a DC50 of 5.7 nM and a Dmax of 90%. This compound demonstrates significant antiproliferative effects in the MOLM-14 cell line, making it a valuable tool for research into the modulation of CK1α activity and its implications in various biological processes and diseases. -
IKZF1/3 And CSNK1A1 Molecular Glue Degrader
MI-2-80 is a molecular glue degrader that specifically targets IKZF1 and IKZF3, as well as CSNK1A1. This compound facilitates the binding of these proteins to the cereblon (CRBN) E3 ubiquitin ligase, promoting their subsequent ubiquitination and proteasomal degradation. MI-2-80 is valuable for research applications focused on understanding the functional roles of IKZF proteins and their involvement in various pathologies, including hematological malignancies. -
STAT6 Molecular Glue
STAT6 degrader-1 is a bifunctional molecular glue that specifically targets STAT6 by recruiting E3 ubiquitin ligase, leading to the proteasomal degradation of the protein. This degradation mechanism allows for the modulation of STAT6 activity, making it a valuable tool in the study of cancer biology, inflammatory diseases, and colorectal cancer. Researchers can utilize STAT6 degrader-1 to explore therapeutic strategies aimed at disrupting STAT6 signaling pathways. -
Molecular Glue Degrader
VNPP433-3β hydrochloride functions as a molecular glue degrader, targeting the androgen receptor (AR) and its splice variants, as well as MAP kinase-interacting serine/threonine protein kinases Mnk1 and Mnk2. This compound promotes apoptosis in cancer cells and has demonstrated efficacy in inhibiting tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β hydrochloride is suitable for research applications focused on castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
Molecular Glue Degrader
VNPP433-3β dihydrochloride is a potent molecular glue degrader that targets the androgen receptor (AR), AR splice variants (AR-Vs), and MAP kinase-interacting serine/threonine protein kinases Mnk1/2. This compound induces apoptosis in cancer cells and has been shown to inhibit tumor growth in CWR22Rv1 xenograft mouse models. VNPP433-3β dihydrochloride is valuable for research in castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
Molecular Glue Degrader
Galeterone hydrochloride is a potent molecular glue degrader that targets the androgen receptor (AR) and its splice variants, as well as MAP kinase-interacting serine/threonine protein kinases Mnk1/2. This compound also acts as a CYP17 inhibitor with an IC50 of 47 nM, promoting cell apoptosis and inhibiting tumor growth in human prostate cancer xenograft models. Galeterone hydrochloride is relevant in the research of castration-resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC). -
Molecular Glue
eEF2K degrader-2 is a molecular glue that targets the eEF2K protein, effectively mediating its degradation. This compound demonstrates significant biological activity by inhibiting proliferation, migration, and invasion, as well as inducing apoptosis in triple negative breast cancer (TNBC) cells. eEF2K degrader-2 exhibits minimal organ toxicity and pathological damage, making it a valuable tool for research applications focused on cancer biology, particularly in breast cancer studies. -
Lck Molecular Glue Degrader
LCK degrader-2 is a Lck molecular glue degrader designed to selectively target and degrade the Lck protein. This compound demonstrates potent biological activity in disrupting Lck-mediated signaling pathways, making it a valuable tool for studying acute lymphoblastic leukemia (ALL) and other Lck-dependent malignancies. Its application in cancer research provides insights into therapeutic strategies for Lck-related diseases. -
Molecular Glue
Lck degrader-1 is a molecular glue degrader that targets lymphocyte-specific protein tyrosine kinase (LCK) with a DC50 of 23.1 nM. This compound plays a significant role in the degradation of LCK, making it a valuable tool for studying T-cell acute lymphoblastic leukemia (T-ALL). Researchers can utilize Lck degrader-1 to explore the molecular mechanisms underlying T-ALL and investigate potential therapeutic strategies. -
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.
