Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC BTK Degrader
DD-03-171 is a selective PROTAC BTK degrader that targets Bruton's tyrosine kinase (BTK) for degradation. This compound demonstrates significant anti-proliferative effects on mantle cell lymphoma (MCL) cells with an IC50 of 5.1 nM and enhances survival in murine models bearing patient-derived xenograft (PDX) lymphoma. Additionally, DD-03-171 inhibits platelet function and thrombosis, making it a valuable tool for research in cancer and hematological disorders. -
Ligands for Target Protein for PROTAC
BTK ligand 12 is a potent ligand for Bruton's tyrosine kinase (BTK), functioning as a valuable component in the development of PROTACs targeting this protein. It exhibits strong binding affinity, facilitating the effective ubiquitination and degradation of BTK in various cellular contexts. This compound is essential for researchers investigating targeted protein degradation and the modulation of signaling pathways associated with BTK in therapeutic applications. -
PROTAC BTK Degrader
PROTAC BTK Degrader-6 is a potent PROTAC degrader targeting Bruton's tyrosine kinase (BTK) with a DC50 of 3.18 nM. This compound exhibits anti-inflammatory activity by inhibiting NF-κB activation and reducing the expression of pro-inflammatory cytokines, including IL-1β and IL-6. It serves as a valuable tool for research into the modulation of immune responses and the development of therapies for inflammatory diseases. -
BTK PROTAC Degrader
UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM, specifically designed to target Bruton's tyrosine kinase (BTK). It effectively disrupts B-cell receptor signaling and demonstrates robust degradation of both wild-type and mutant BTK proteins, including the C481S mutation. UBX-382 has been shown to inhibit tumor growth in murine xenograft models with BTK-expressing TMD-8 cells, making it a valuable tool for investigating B-cell-related malignancies and therapeutic strategies. -
BTK PROTAC Degrader
PROTAC BTK Degrader-2 is a highly effective proteolysis-targeting chimera (PROTAC) that selectively degrades Bruton's tyrosine kinase (BTK). By recruiting the Cullin-RING E3 ubiquitin ligase complex, it mediates the ubiquitination and subsequent degradation of BTK protein, leading to a marked reduction in its cellular levels. This compound is valuable in research focused on B-cell malignancies and autoimmune diseases, providing insights into BTK's role in signaling pathways and therapeutic interventions. -
PROTAC BTK Degrader
PROTAC BTK Degrader-10 is a PROTAC agent that targets Bruton's Tyrosine Kinase (BTK) for selective degradation. This compound is particularly useful in the study of chronic lymphocytic leukemia (CLL) due to its ability to modulate BTK levels, thereby influencing malignant cell survival and proliferation. The degrader is designed with a specific ligand for BTK and a linker, enabling effective recruitment of the E3 ubiquitin ligase Cereblon for targeted degradation. -
PROTAC Btk Degrader
SJF620 hydrochloride functions as a PROTAC designed for the degradation of Bruton's tyrosine kinase (Btk) via recruitment of the cereblon (CRBN) E3 ligase. With a DC50 value of 7.9 nM, SJF620 effectively mediates the targeted degradation of Btk, making it a valuable tool for research focused on Btk-related pathways. This compound is particularly relevant in studies of immune responses and various hematological malignancies. -
PROTAC BTK Degrader
PTD10 is a potent PROTAC degrader targeting Bruton's tyrosine kinase (BTK), exhibiting a DC50 of 0.5 nM and a KD of 2.28 nM. It effectively degrades BTK in Ramos and JeKo-1 cell lines, leading to the inhibition of cell growth and the induction of apoptosis through caspase activation and mitochondrial pathways. PTD10 is suitable for investigating mechanisms of B-cell dysregulation and related therapeutic strategies. -
BTK PROTAC Degrader
DDa-1 is a potent BTK PROTAC degrader with a DC50 of 90 nM, designed to facilitate the targeted degradation of Bruton's Tyrosine Kinase (BTK) in cellular systems. This compound effectively utilizes a novel mechanism involving DCAF1 binding, a distinct linker, and a specific BTK ligand to enhance selectivity and efficacy. DDa-1 is primarily utilized in research applications focusing on BTK-related signaling pathways and therapeutic strategies against B-cell malignancies. -
PROTAC BTK Degrader
BCPyr is a PROTAC-class degrader specifically targeting Bruton’s Tyrosine Kinase (BTK), exhibiting a DC50 of 800 nM. This compound integrates a BTK ligand (ligand 11) and an E3 ubiquitin ligase ligand (ligand 20) through a pyrazinyl methanol linker. BCPyr facilitates the targeted degradation of BTK, making it a valuable tool for studying diseases where BTK is implicated, such as certain hematological malignancies. -
BTK/IKZF1/3 PROTAC Ligand
BTK/IKZF1/3 ligand 1 is a PROTAC ligand targeting Bruton's tyrosine kinase (BTK) and the Ikaros family zinc finger proteins (IKZF1/3). This compound can be conjugated with E3 ligase ligands and linkers to produce PROTAC BTK/IKZF1/3 Degrader-1, facilitating targeted protein degradation. It is valuable for cancer research, supporting investigations into therapeutic strategies aimed at modulating BTK and IKZF1/3 activity in malignant cells. -
BTK PROTAC Degrader
PROTAC BTK Degrader-12 is a PROTAC (Proteolysis Targeting Chimera) designed to selectively degrade Bruton's tyrosine kinase (BTK). It facilitates the targeted ubiquitination and subsequent proteasomal degradation of BTK, resulting in diminished signaling pathways associated with B-cell malignancies and autoimmune disorders. This compound serves as a valuable tool in research investigating BTK's role in disease mechanisms and therapeutic interventions. -
BTK PROTAC Degrader
TQ-3959 is an orally bioavailable BTK PROTAC degrader that demonstrates a DC50 of 14.6 nM. It exhibits potent antiproliferative effects on both wild-type BTK and the C481S mutant BTK cell lines. In vivo, TQ-3959 effectively inhibits tumor growth in female NOD-SCID mice bearing TMD-8 xenografts. This compound is valuable for investigating B-cell malignancies, including lymphoma. -
BTK/IKZF1/3 PROTAC Degrader
PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally bioavailable degrader targeting BTK, IKZF1, and IKZF3 through the PROTAC mechanism. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research, particularly in the context of lymphoma. Its unique mechanism of action allows for the targeted degradation of specific oncogenic proteins, facilitating studies in therapeutic strategies and disease mechanisms. -
PROTAC BTK Degrader
PROTAC BTK Degrader-4 is a highly effective PROTAC designed to selectively degrade Bruton's tyrosine kinase (BTK) with a DC50 of less than 100 nM. This compound demonstrates minimal immunomodulatory imide drug (IMiD) activity, with a DC50 of 0.345 μM and a maximum degradation rate of 27.4%. PROTAC BTK Degrader-4 is suitable for investigating various pathologies, including cancers, autoimmune disorders, and inflammatory diseases associated with BTK dysregulation. -
BTK PROTAC Degrader
PROTAC BTK Degrader-3 is a selective degrader targeting Bruton's tyrosine kinase (BTK) with a DC50 value of 10.9 nM for BTK degradation in Mino cells. This compound demonstrates significant biological activity and is applicable in research focusing on B-cell malignancies, particularly chronic lymphoid malignancies. Its mechanism of action offers potential pathways for therapeutic intervention in relevant disease models. -
BTK PROTAC Degrader
PROTAC BTK Degrader-14 is a targeted protein degrader that specifically degrades Bruton's tyrosine kinase (BTK) through the PROTAC mechanism of action. This compound is significant in cancer research, particularly for studies focused on malignancies where BTK plays a crucial role in signaling pathways. Its ability to effectively modulate BTK levels can provide insights into therapeutic strategies and disease mechanisms involving this key protein. -
PROTAC ALK Degrader
SIAIS001 is a potent PROTAC degrader targeting anaplastic lymphoma kinase (ALK) with a DC50 of 3.9 nM. This compound induces G1/S phase cell cycle arrest and effectively inhibits the proliferation of SR cells with an IC50 of 0.9 nM. SIAIS001 is suitable for research in non-small cell lung cancer (NSCLC) and anaplastic large-cell lymphomas (ALCLs). -
NPM-ALK PROTAC Degrader
MS99-β-Gal is a galactose-modified PROTAC degrader targeting the NPM-ALK fusion protein. This compound is selectively hydrolyzed by SA-β-gal and esterase in senescent cancer cells, allowing the release of MS99, which effectively degrades the NPM-ALK protein. MS99-β-Gal demonstrates an IC50 of 454.8 nM in aging Karpas 299 cells, showing improved potency compared to normal Karpas 299 cells with an IC50 of 2.162 μM. This reagent is valuable for cancer research, particularly in studies focused on targeted protein degradation. -
Ligands for Target Protein for PROTAC
ALK protein ligand-1 is a specific ligand for anaplastic lymphoma kinase (ALK) that plays a crucial role in targeted protein degradation using PROTAC technology. This compound exhibits potent inhibitory effects on ALK, making it a valuable tool for studying ALK-related signaling pathways and their implications in cancer biology. ALK protein ligand-1 is essential for the synthesis of AP-1, facilitating the exploration of novel therapeutic approaches in oncology research. -
EML4-ALK PROTAC Degrader
PROTAC EML4-ALK Degrader-2 is an advanced degrader specifically targeting the EML4-ALK fusion protein. With an IC50 of 1.6 nM, it exhibits potent selective inhibitory activity against ALK while maintaining selectivity over IGF1R, INSR, FLT3, and FGFR2. This compound demonstrates significant anti-cancer effects in both in vitro and in vivo models and is particularly relevant for research applications involving non-small cell lung cancer (NSCLC), as well as liver and cervical cancers. -
Brigatinib-PROTAC Degrader
SIAIS117 is a potent Brigatinib-PROTAC degrader that targets the ALK protein, specifically effective against the ALK G1202R point mutation. By utilizing a VHL-1 conjugation, SIAIS117 exhibits significant capability to induce protein degradation, leading to inhibited growth of SR and H2228 cancer cell lines. This compound holds potential for applications in anti-proliferative research, particularly in small cell lung cancer contexts. -
ALK PROTAC Degrader
PROTAC ALK degrader-5 is a targeted degrader composed of a small molecule that selectively degrades anaplastic lymphoma kinase (ALK). It demonstrates potent inhibitory activity against EML4-ALK and NPM-ALK, with IC50 values of 27.4 nM and 116.5 nM, respectively. This compound exhibits significant anti-proliferative effects against ALK-driven cancer cell lines, including H3122 and Karpas 299, and effectively inhibits ALK and STAT3 phosphorylation. PROTAC ALK degrader-5 is a valuable tool for investigating ALK-driven malignancies, particularly in the context of human non-small cell lung cancer and anaplastic large cell lymphoma research. -
ALK PROTAC Degrader
TD-004 is a highly effective ALK PROTAC degrader, demonstrating potent anti-ALK inhibitory activity with an IC50 of 0.11 µM. This compound selectively hampers the proliferation of ALK-positive cancer cell lines, SU-DHL-1 and H3122, with IC50 values of 0.058 µM and 0.28 µM, respectively. TD-004 induces the degradation of ALK fusion proteins, including NPM-ALK and EML4-ALK, through the recruitment of the VHL E3 ligase and the proteasome pathway. Its significant tumor growth inhibition and favorable safety profile in vivo make TD-004 a valuable tool for researching anaplastic large cell lymphoma and non-small cell lung cancer. -
AURKA PROTAC Degrader
SK2187 is a selective degrader of Aurora kinase A (AURKA) utilizing the PROTAC technology, exhibiting a DC50 of approximately 10 nM. This compound demonstrates significant growth inhibition of NGP neuroblastoma cells, with an IC50 value of 101.5 nM. SK2187 is particularly relevant for research on MYCN-amplified neuroblastoma, enabling exploration of targeted degradation pathways in cancer therapy. -
Aurora-A/Aurora-B PROTAC Degrader
dAurAB2 is a dual-targeting PROTAC designed to degrade Aurora-A and Aurora-B, demonstrating potent efficacy with DC50 values of 59 nM and 39 nM, respectively. This compound effectively reduces N-Myc protein levels in MYCN-amplified IMR32 neuroblastoma cells, making it a valuable tool for neuroblastoma research. The unique design incorporates a specific Aurora ligand and an E3 ligase ligand connected by a tailored linker, facilitating targeted degradation and advancing studies in cancer biology. -
Aurora A PROTAC Degrader
AurAP14 is a PROTAC degrader specifically targeting Aurora A, with a DC50 of 120 nM. This compound exhibits potent inhibitory effects on various tumor cell lines, showing IC50 values of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis while effectively arresting A549 cells in the S and G2/M phases of the cell cycle. Additionally, AurAP14 demonstrates significant anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR, making it a valuable tool for research focused on treating Aurora A-overexpressing non-small cell lung cancer (NSCLC). -
Aurora A PROTAC Degrader
PROTAC Aurora A Degrader-1 is a selective degrader that targets Aurora A, effectively forming a ternary complex with AURKA and CRBN. This compound demonstrates potent biological activity, inducing degradation of AURKA, lowering MYCN levels, and promoting DNA damage and apoptosis in cancer cells. With DC50 values of 1 nM and 2 nM in LAN5 and SMS-SAN cells, respectively, it exhibits significant antiproliferative effects and is valuable for research on neuroblastoma and small cell lung cancer. -
BRD4 PROTAC Degrader
PROTAC BRD4 Degrader-21 is a targeted PROTAC that degrades the BRD4 protein through the induction of ubiquitination, achieving an IC50 of 59 nM. This compound effectively leads to BRD4 degradation via the proteasome pathway, and demonstrates moderate affinity for recombinant HSP90α with an IC50 range of 100-1000 nM. In preclinical studies, PROTAC BRD4 Degrader-21 has been shown to induce apoptosis in cancer cells and inhibit tumor growth in xenograft mouse models, making it a valuable tool for research into acute myeloid leukemia and diffuse large B-cell lymphoma. -
TNF-alpha inhibitor
Pomalidomide is a derivative of thalidomide and acts as an immunomodulator. -
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.
