Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Hemagglutinin Degrader
PROTAC Hemagglutinin Degrader-1 is a potent degrader specifically targeting influenza hemagglutinin (HA). It exhibits significant biological activity with a median degradation concentration of 1.44 μM, demonstrating broad-spectrum efficacy against influenza viruses. This compound is valuable for research applications focused on viral suppression and the development of antiviral therapeutic strategies. -
HIV-1 Nef Binder, IKZF1 Modulator
FC-14369 is a PROTAC degrader that selectively targets the HIV-1 Nef protein, exhibiting a DC50 value of 160 nM. By engaging both Nef and the Cereblon E3 ubiquitin ligase, FC-14369 facilitates the ubiquitination and subsequent proteasomal degradation of Nef, leading to the restoration of CD4 and MHC-I expression on the cell surface and effectively inhibiting HIV-1 replication. This compound is valuable for research focused on HIV infection and AIDS, advancing understanding of therapeutic strategies in viral infections. -
PROTAC linker
Cl-C6-PEG4-O-CH2COOH (PROTAC Linker 4) is a PROTAC linker can be used in the synthesis of chloroalkane-containing PROTACs (HaloPROTACs). -
PROTAC linker
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a small molecule HaloPROTAC that incorporates the VH032 based VHL ligand and 5-unit PEG linker. -
PROTAC linker
Pomalidomide-PEG4-C-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology. -
E3 ligase ligand-linker conjugate
Thalidomide-O-amido-PEG2-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology. -
E3 ligase ligand-linker conjugate
Thalidomide-O-amido-C6-NH2 TFA (Cereblon Ligand-Linker Conjugates 11 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. -
E3 ligase ligand-linker conjugate
(S,R,S)-AHPC-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology. -
E3 ligase ligand-linker conjugate
(S,R,S)-AHPC-PEG2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in PROTAC technology. -
E3 ligase ligand-linker conjugate
(S,R,S)-AHPC-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. -
E3 ligase ligand-linker conjugate
cIAP1 Ligand-Linker Conjugates 11 Hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 11 Hydrochloride can be used to design SNIPERs. -
E3 ligase ligand-linker conjugate
cIAP1 Ligand-Linker Conjugates 15 hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 hydrochloride can be used to design SNIPERs. -
E3 ligase ligand-linker conjugate
Pomalidomide-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology. -
E3 ligase ligand-linker conjugate
Thalidomide-O-amido-C3-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. -
CRBN modulator
CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM. -
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. - (S,R,S)-AHPC , also known as also known as MDK7526; VHL Ligand 1; Protein degrader 1, is a potent and selective protein degrader. MDK7526 is potential useful for the targeted degradation of the androgen receptor.
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PROTAC degrader
SNIPER(CRABP)-11, also known as PROTAC cIAP1 degrader-4, is a potent protein degrader.
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PROTAC B-Raf Degrader
PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) that facilitates the degradation of B-Raf through a Cereblon ligand. This compound demonstrates significant anti-cancer activity, making it a valuable tool for cancer research. It is particularly useful in studies investigating B-Raf-mediated signaling pathways and therapeutic strategies targeting oncogenic mutations in B-Raf. -
SMARCA2 Degrader
ACBI2 is a potent VHL PROTAC designed for the targeted degradation of SMARCA2. With an EC50 of 7 nM and a DC50 of 1 nM in RKO cells, ACBI2 selectively modulates SMARCA2 levels, making it a valuable tool for studying SMARCA2-related pathways. This compound is particularly relevant in lung cancer research, facilitating investigations into therapeutic strategies targeting SMARCA2 degradation. -
AR-V7 PROTAC Degrader
PROTAC AR-V7 degrader-1 is a selective degrader targeting the androgen receptor variant 7 (AR-V7) through the PROTAC mechanism. With a DC50 of 0.32 μM in 22Rv1 cells, this compound demonstrates potent inhibition of tumor cell proliferation and exhibits significant anti-tumor activity. It is particularly relevant for research applications focusing on prostate cancer and can aid in the development of targeted therapeutic strategies. -
EZH2 Degrader
MS8815 is a selective enhancer of the enhancer of zeste homolog 2 (EZH2) and functions as a PROTAC degrader. With an IC50 value of 8.6 nM, MS8815 demonstrates potent inhibitory activity against EZH2. This compound is valuable for research applications focused on triple-negative breast cancer (TNBC) and other conditions influenced by EZH2 activity. -
KRAS G12D PROTAC Degrader
Setidegrasib is a PROTAC degrader specifically targeting the KRAS G12D mutation with a DC50 of 37 nM. This compound effectively induces the degradation of KRAS G12D protein, leading to the suppression of key signaling molecules such as p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates significant anti-tumor activity across various cancer xenograft models, making it a valuable tool for studying KRAS(G12D)-mutated solid tumors. -
BLC6 PROTAC Degrader
ARV-393 is a potent BCL6 PROTAC degrader that facilitates the ubiquitination and subsequent proteasomal degradation of BCL6. This compound exhibits significant biological activity and is particularly relevant for research focused on advanced non-Hodgkin lymphoma. Its ability to modulate protein levels through targeted degradation makes it a valuable tool for elucidating BCL6-related pathways in cancer biology. -
JAK2/3 PROTAC Degrader
SJ10542 is a potent and selective PROTAC degrader targeting JAK2 and JAK3. With DC50 values of 14 nM for JAK2 and 11 nM for JAK3 in patient-derived xenograft cells (PDX), SJ10542 demonstrates significant antitumor activity. This compound is valuable for research in hematological malignancies and autoimmune diseases, facilitating the exploration of targeted degradation mechanisms in these therapeutic areas. -
PROTAC BRD4 Degrader
GAL-02-221 is a PROTAC designed to target and degrade BRD4 through ligands that recruit von Hippel-Lindau (VHL) E3 ligase. This compound effectively promotes the degradation of BRD4 in both HER2-positive and negative breast cancer cell lines, demonstrating potential utility in the study of tumor biology and therapeutic approaches. Its ability to selectively eliminate BRD4 highlights its relevance in cancer research and provides a valuable tool for investigating mechanisms of oncogenesis and treatment resistance. -
PROTAC FKBP12 Degrader
FKBP12 PROTAC RC32 is a targeted protein degrader utilizing PROTAC technology to selectively degrade FKBP12. This compound combines Rapamycin, a well-characterized immunosuppressant, with a Cereblon E3 ubiquitin ligase ligand derived from Pomalidomide, facilitating the ubiquitination and subsequent proteasomal degradation of FKBP12. It serves as an important tool in research applications aimed at investigating the modulation of protein levels and the functional consequences of targeted degradation in various biological contexts. -
AKT PROTAC Degrader
MS21 is a potent AKT PROTAC degrader designed to selectively target and degrade AKT proteins. This compound effectively inhibits mutations within the PI3K/PTEN pathway, leading to suppressed tumor cell proliferation and induction of cell cycle arrest. MS21 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development.
