Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC ERα Degrader
PROTAC ERα Degrader-4 is a selective degrader targeting estrogen receptor alpha (ERα) through the PROTAC mechanism. It exhibits potent inhibitory activity with a Ki value of 5.08 μM, effectively leading to the degradation of ERα in both Tamoxifen-sensitive and resistant ER+ breast cancer cells, as well as in ERα-mutated breast cancer cell lines. Additionally, PROTAC ERα Degrader-4 induces apoptosis, making it a valuable tool for cancer research aimed at understanding and combating ERα-driven malignancies. -
PROTAC HDAC8 Degrader
SZUH280 is a selective PROTAC degrader targeting HDAC8, demonstrating a DC50 of 0.58 μM in A549 cells. It effectively induces apoptosis in cancer cells and disrupts DNA repair mechanisms, thereby enhancing cellular radiosensitivity. This compound is particularly useful for research related to cancer therapeutics and the study of epigenetic regulation. -
PROTAC eEF2K Degrader
PROTAC eEF2K degrader-1 is a small molecule designed to target and induce degradation of the elongation factor 2 kinase (eEF2K). This compound has been shown to effectively promote apoptosis in MDA-MB-231 cancer cells, demonstrating its potential in cancer research. The mechanism of action involves the targeted elimination of eEF2K, providing a valuable tool for studying the role of this kinase in cellular processes and therapeutic applications. -
PROTAC XPO1 Degrader
PROTAC XPO1 degrader-1 is a targeted protein degrader designed to selectively promote the degradation of XPO1. This compound demonstrates significant anti-proliferative effects, induces apoptosis, inhibits NF-κB signaling, and causes cell cycle arrest at the G1 phase. It is an important tool for researching hematological malignancies, offering insights into therapeutic strategies by modulating XPO1 levels. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4 degrader-38 is a dual-targeted PROTAC degrader designed to promote the ubiquitination and subsequent degradation of the SMARCA2 and SMARCA4 proteins. With DC50 values of 3.0 nM and 4.0 nM for SMARCA2 and SMARCA4 respectively, this compound effectively blocks the G0/G1 cell cycle phase and induces apoptosis in cancer cells. It has significant potential for use in research focused on acute myeloid leukemia (AML) and other malignancies involving these chromatin remodeling factors. -
PROTAC JAK2 Degrader
SJ1008030 is a PROTAC compound designed to selectively degrade Janus kinase 2 (JAK2). This compound exhibits potent inhibitory activity against MHH–CALL-4 cell growth, with an IC50 of 5.4 nM. SJ1008030 is valuable for research applications focusing on leukemia, facilitating the study of JAK2-related pathways and therapeutic interventions. -
PROTAC FLT3/JAK2/BRD4 Degrader
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a potent PROTAC degrader that simultaneously targets FLT3, JAK2, and BRD4, exhibiting DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It demonstrates significant antiproliferative activity against MV4;11 cells with an IC50 of 0.79 nM, inducing apoptosis in these cells. Additionally, PROTAC FLT3/JAK2/BRD4 Degrader-1 shows marked anti-tumor efficacy in MV4;11 xenograft models in NOD SCID mice. This compound is valuable for research into acute myeloid leukemia (AML). -
PROTAC FGFR1/2 Degrader
DGY-09-192 is a PROTAC degrader targeting FGFR1 and FGFR2, demonstrating DC50 values of 4.35 nM and 70 nM, respectively. This compound selectively degrades both wild-type FGFR1/2 and various FGFR2 fusion proteins, such as FGFR2-PHGDH and FGFR2-OPTN. By suppressing downstream FGFR signaling, DGY-09-192 effectively reduces the phosphorylation of key targets including FRS2 Y196 and ERK1/2 T202/Y204, making it a valuable tool for investigating FGFR-driven malignancies in both in vitro and in vivo studies. -
PROTAC GPX4 Degrader
PROTAC GPX4 degrader-5 is a selective degrader targeting GPX4, with a DC50 of 28 nM. This compound effectively induces ferroptosis and enhances reactive oxygen species (ROS) levels while exhibiting low toxicity to normal cells. PROTAC GPX4 degrader-5 demonstrates significant anti-proliferative effects in various tumor cell lines, making it a valuable tool for cancer research. -
KRASG12D PROTAC Degrader
PROTAC K-Ras Degrader-5 is a cereblon-based PROTAC specifically designed to target KRASG12D, achieving a DC50 of less than 100 nM. This reagent facilitates the recruitment of KRASG12D to the cereblon E3 ubiquitin ligase complex, leading to its ubiquitination and proteasomal degradation. As a result, it effectively reduces pERK levels and inhibits the proliferation of cancer cells. PROTAC K-Ras Degrader-5 also enhances caspase 3/7 activity and cleaved PARP levels, indicative of apoptosis, in pancreatic cancer models. This compound is a valuable tool for researching both pancreatic and colorectal cancer. -
Multiple Target PROTAC
GT19630 is a multiple target PROTAC designed to degrade c-MYC, CK1α, GSPT1, and IKZF1/2/3 proteins. This compound effectively targets and reduces the levels of these proteins in various tumor cell lines, making it a valuable tool for studying diseases characterized by high c-MYC expression, including cancer, cardiovascular disorders, cerebrovascular diseases, and viral infections. Researchers can utilize GT19630 to further investigate the therapeutic potential of protein degradation in relevant biological contexts. -
HPK1 PROTAC Degrader
PROTAC HPK1 Degrader-5 is a highly potent and orally bioavailable PROTAC that targets HPK1 for degradation (DC50 = 5.0 nM; Dmax ≥ 99%). This compound effectively inhibits SLP76 phosphorylation and promotes ERK pathway activation, leading to increased release of IL-2 and IFN-γ. It demonstrates the capability to counteract immunosuppressive signals induced by PGE2, NECA, or TGF-β. Additionally, PROTAC HPK1 Degrader-5 has shown efficacy in inhibiting tumor growth in MC38 syngeneic mouse models, making it a valuable tool for research in tumor immunotherapy, particularly in colorectal cancer. -
IRAK4 PROTAC Degrader
PROTAC IRAK4 degrader-14 is an orally active degrader targeting IRAK4 with a DC50 of 2.4 nM. It functions by selectively degrading IRAK4, thereby inhibiting pro-inflammatory responses in various cell types, including T cells, monocytes, and keratinocytes. This compound has significant relevance in research focused on inflammatory diseases, particularly psoriasis. -
DcpS PROTAC degrader
JCS-1 is a highly potent DcpS PROTAC degrader that facilitates the targeted degradation of the DcpS enzyme through non-covalent binding via a RG3039-based warhead, while recruiting the E3 ligase VHL. This compound effectively promotes ubiquitination and subsequent degradation of DcpS at nanomolar concentrations, demonstrating a DC50 value of 87 nM in MOLM-14 cells. JCS-1 is a valuable tool for investigating acute myeloid leukemia (AML) and other genetic disorders associated with DcpS dependency. -
PTPN2 PROTAC Degrader
PROTAC PTPN2 degrader-2 TFA is a highly potent PTPN2 degrader with a DC50 of less than 50 nM. This compound facilitates targeted protein degradation, providing a valuable tool for investigating the role of PTPN2 in cancer and metabolic disorders, including colon cancer. Its application in research can enhance understanding of disease mechanisms and therapeutic interventions. -
PTPN2 PROTAC Degrader
PROTAC PTPN2 Degrader-2 is a selective PTPN2 degrader that effectively induces targeted degradation of the PTPN2 protein, demonstrating a DC50 of less than 50 nM. This compound is instrumental for exploring cellular mechanisms within cancer and metabolic disorders, particularly in the context of colon cancer research. Its utility in protein knockdown enables innovative studies into therapeutic strategies for disease intervention. -
STAT6 PROTAC Degrader
PROTAC STAT6 degrader-1 is a targeted protein degradative compound designed to modulate STAT6 activity through the recruitment of E3 ligase CRBN. With a DC50 of less than 1 nM, this PROTAC showcases potent efficacy in STAT6 degradation. It is particularly relevant for research on inflammation and various cancer types, providing a valuable tool for exploring STAT6's role in pathophysiology and therapeutic responses. -
STAT3 PROTAC Degrader
SD-436 is a selective and potent degrader of STAT3, functioning through the PROTAC mechanism with a DC50 of 0.5 μM and an IC50 of 19 nM for STAT3. It promotes the ubiquitination and subsequent degradation of STAT3, leading to significant tumor regression. This reagent is applicable in cancer research, including studies focused on leukemia and lymphoma. -
PTP1B/TC-PTP PROTAC Degrader
DU-14 is a potent dual degrader targeting PTP1B and TC-PTP via the PROTAC mechanism. It demonstrates remarkable selectivity with IC50 values of 24.2 nM and 30.1 nM for PTP1B and TC-PTP phosphatase activity, respectively. DU-14 enhances interferon-gamma signaling, promotes T cell activation, and exhibits anti-tumor properties, making it a valuable tool for cancer immunology research and the study of immune modulation. -
STAT6 PROTAC Degrader
PROTAC STAT6 degrader-3 is a highly potent degrader targeting STAT6, exhibiting a DC50 of less than 1 nM. This compound facilitates the targeted degradation of STAT6, making it a valuable tool for investigating allergic and inflammatory diseases as well as various cancers. Its application in research can provide insights into the role of STAT6 in disease pathways and therapeutic interventions. -
STAT3 PROTAC Degrader
SD-2301 is a selective STAT3 PROTAC degrader that targets and induces the degradation of STAT3 while preserving the expression of other STAT family members such as STAT1, STAT2, STAT4, STAT5, and STAT6. It has demonstrated anti-tumor efficacy in B16F10-bearing mouse models, making it a valuable tool for cancer research. This compound can be utilized in studies focused on the modulation of STAT3 pathways and the development of targeted therapies. -
PROTAC STAT6 Degrader
PROTAC STAT6 Degrader-2 is a potent bifunctional degrader that specifically targets signal transducer and activator of transcription 6 (STAT6). It demonstrates high efficiency with a DC50 of 1-10 nM in human peripheral blood mononuclear cells (PBMC) and less than 100 nM in HEK293-HIBiT-STAT6 cells. This compound is ideal for research applications related to STAT6-mediated diseases, facilitating the study of its role in various biological processes. -
STAT6 PROTAC Degrader
PROTAC STAT6 degrader-4 is a potent STAT6 PROTAC degrader with a DC50 of 0.04 nM. It functions by inducing the ubiquitination and subsequent degradation of STAT6, making it an important tool for investigating immune-related diseases. This compound is valuable for researchers studying the role of STAT6 in immune signaling pathways and therapeutic interventions. -
PROTAC STAT3 Degrader
S3D5 is a selective PROTAC degrader specifically targeting STAT3, with a dissociation constant (KD) of 4.35 μM. It effectively induces degradation of the STAT3 protein in HepG2 cells, demonstrating minimal impact on other STAT proteins. This degradation is mediated via the ubiquitin-proteasome system, contributing to its potent anti-proliferative effects in hepatocellular carcinoma by activating the p53 pathway. S3D5 serves as a valuable tool for research focused on the mechanisms underlying hepatocellular carcinoma. -
PROTAC ERK5 Degrader
PPM-3 is a potent and selective PROTAC degrader of ERK5, exhibiting an IC50 of 62.4 nM. While PPM-3 does not directly affect tumor cell proliferation, it modulates tumor development by impacting macrophage differentiation. This compound may serve as a valuable tool for investigating the role of ERK5 degradation in cancer biology and immune modulation. -
BCR-ABL PROTAC Degrader
Leu-PEG1-Dasa is an efficient BCR-ABL PROTAC degrader that operates through the N-terminal canonical pathway, demonstrating a DC50 of 0.48 nM. This compound utilizes a single amino acid as the E3 ligase ligand and exhibits significant anti-proliferative effects on K562 cells. Leu-PEG1-Dasa is applicable in the research of chronic myeloid leukemia (CML) and provides insights into targeted degradation mechanisms in cancer therapy. -
BCR-Abl PROTAC Degrader
GMB-805 is a potent BCR-Abl PROTAC degrader, demonstrating a DC50 of 30 nM in K562 cells. It effectively induces antiproliferative activity, making it a valuable tool for studying chronic myeloid leukemia. Additionally, GMB-805 exhibits significant anti-tumor efficacy in vivo, coupled with a favorable safety profile, highlighting its potential for therapeutic development. -
mini-PROTAC BCR-ABL Degrader
Arg-PEG1-Dasa is a mini-PROTAC designed to selectively degrade BCR-ABL, a key oncogenic driver in chronic myeloid leukemia. It demonstrates potent degradation efficacy with an EC50 of 0.85 nM, and exhibits significant antiproliferative activity in K562 cells, with an IC50 of 0.36 nM. This reagent is valuable for research applications focused on targeted therapies for BCR-ABL-driven malignancies. -
PROTAC degrader
P19As is a PROTAC degrader that targets the BCR-ABL fusion protein, exhibiting a DC50 value of approximately 200 nM for wild-type BCR-ABL. This compound effectively degrades the T315I mutant variant and demonstrates potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cell lines. P19As serves as a valuable tool for investigating therapeutic strategies in chronic myeloid leukemia and acute lymphoblastic leukemia. -
BCR-ABL PROTAC Degrader
P19P is a BCR-ABL PROTAC degrader that demonstrates a DC50 value of approximately 20 nM for wild-type BCR-ABL protein. It effectively degrades various drug-resistant mutants, including T315I, E255K, H396R, and V468F, and exhibits significant anti-proliferative activity in BaF3-BCR-ABL (T315I) cells, with an IC50 of 13.1 nM against ABL (T315I). P19P is suitable for research applications related to chronic myeloid leukemia and acute lymphoblastic leukemia while showing no inhibition of vascular lumen formation in HUVEC cells. -
BCR-ABL PROTAC Degrader
SIAIS100 is a potent BCR-ABL PROTAC degrader, exhibiting a DC50 value of 2.7 nM. This compound facilitates the targeted degradation of the BCR-ABL fusion protein, making it an important tool in the study of chronic myeloid leukemia (CML). Its ability to induce proteolytic degradation offers valuable insights for therapeutic development and understanding disease mechanisms associated with CML. -
BCR-ABL PROTAC Degrader
SIAIS056 is a BCR-ABL PROTAC degrader that effectively targets and degrades BCR-ABL fusion proteins, displaying a potent DC50 value of 0.18 nM. It inhibits the BCR-ABL signaling pathway in a time-dependent manner, leading to reduced phosphorylation of BCR-ABL as well as downstream effectors like STAT5 and CRKL in K562 cells. Additionally, SIAIS056 demonstrates the ability to degrade various BCR-ABL resistance mutations and exhibits significant anti-proliferative effects, resulting in marked tumor regression in K562 xenograft models. This compound is valuable for research in leukemia. -
BCR-ABL PROTAC Degrader
P22D is a BCR-ABL PROTAC degrader designed for targeted protein degradation, exhibiting a DC50 value of approximately 10 nM for the wild-type BCR-ABL protein. This compound effectively inhibits the proliferation of K562 cells harboring the wild-type BCR-ABL, but does not exhibit activity against BaF3-BCR-ABL (T315I) cells. P22D is valuable for research on chronic myeloid leukemia and acute lymphocytic leukemia, offering insights into the mechanisms of resistance and targeted therapies. -
BCR-ABL PROTAC Degrader
Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, demonstrating a DC50 value of 1.56 nM. This compound utilizes phenylalanine as the E3 ligase ligand and triggers the N-end rule pathway to facilitate the degradation of target proteins. Phe-PEG1-Dasa effectively suppresses the proliferation of K562 leukemia cells, making it a valuable tool for research into leukemia treatment strategies. -
PROTAC FLT3-ITD Degrader
PF15 is a PROTAC designed to target FLT3 kinase through its ligands linked with CRBN. This highly selective FLT3-ITD degrader exhibits a DC50 of 76.7 nM, effectively inhibiting the proliferation of FLT3-ITD-positive cells. PF15 down-regulates the phosphorylation of FLT3 and STAT5, demonstrating significant anti-tumor activity in mouse models, making it a valuable tool for leukemia research. -
LCK PROTAC Degrader
SJ11646 is a LCK-targeting PROTAC degrader based on Dasatinib, exhibiting a DC50 of 0.00838 pM. This compound demonstrates potent cytotoxic effects against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples, effectively prolonging LCK signaling suppression and inducing apoptosis in T-ALL. Additionally, SJ11646 binds with high affinity to 51 human kinases, including ABL1, KIT, and DDR1, and shows enhanced antileukemic efficacy in T-ALL mouse models, making it a valuable tool for research into novel therapeutic strategies for leukemia. -
PROTAC CDK4/6/9 Degrader
PROTAC CDK4/6/9 Degrader 1 is a targeted protein degradation agent that specifically degrades cyclin-dependent kinases CDK4, CDK6, and CDK9. This compound effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells by inducing G1 phase arrest, promoting apoptosis, and suppressing cellular migration and invasion. PROTAC CDK4/6/9 Degrader 1 serves as a valuable tool for studying the role of these kinases in TNBC and may support the development of novel therapeutic strategies aimed at this aggressive cancer subtype. -
PROTAC USP7 Degrader
XM-U-14 is a selective PROTAC degrader targeting USP7, demonstrating a DC50 of 0.74 nM for inducing USP7 degradation in the RS4;11 cell line. This compound effectively upregulates p53 and p21 levels and exhibits significant inhibition of acute lymphoblastic leukemia (ALL) cell proliferation, with IC50 values of 0.5 nM and 8.3 nM for RS4;11 and Reh cells, respectively. Additionally, XM-U-14 induces apoptosis and cell cycle arrest, ultimately inhibiting tumor growth, making it a valuable tool for cancer research and therapeutic exploration. -
RET PROTAC Degrader
RD-23 is a selective RET PROTAC degrader that functions through the promotion of ubiquitination and subsequent degradation of the RETG810C mutation, exhibiting a DC50 value of 11.7 nM. This compound effectively inhibits downstream Shc signaling pathways and induces apoptosis in RET-related cancer models. RD-23 is a valuable tool for investigating the biological roles and therapeutic targeting of RET in oncology research. -
EML4-ALK PROTAC Degrader
Pro-PEG3-BA is a targeted PROTAC degrader that specifically degrades EML4-ALK and EGFR mutants, with DC50 values of 0.42 μM and 13.50 μM, respectively. It effectively inhibits proliferation and induces cell cycle arrest and apoptosis in non-small cell lung cancer (NSCLC) cell lines in vitro. In vivo studies reveal that Pro-PEG3-BA rewires the ubiquitin-proteasome system, leading to a reduction in EML4-ALK protein levels while demonstrating a favorable safety profile. This reagent is suitable for research focused on non-small cell lung cancer treatments. -
AR PROTAC Degrader
ITRI-90 is an orally bioavailable androgen receptor (AR) PROTAC degrader that facilitates the degradation of both full-length AR (AR-FL) and the splice variant AR-V7 through the ubiquitin-proteasome pathway. This mechanism effectively reduces AR transcriptional activity and downregulates target gene expression. ITRI-90 has shown significant antitumor effects by inhibiting the proliferation of prostate cancer cells, including those resistant to Enzalutamide, and promoting apoptosis. Additionally, it possesses favorable pharmacokinetic properties, making it a valuable tool for research in prostate cancer. -
BRD4 PROTAC Degrader
NEP162 is a potent BRD4 PROTAC degrader, demonstrating DC50 values of 1.2 and 1.6 μM in SW480 and U2OS cell lines, respectively. It exhibits significant antiproliferative activity, effectively inhibiting tumor growth and promoting apoptosis in various cancer models. NEP162 is particularly relevant for research applications in osteosarcoma, colorectal cancer, and non-small cell lung cancer. -
AR PROTAC degrader
PROTAC AR-NTD degrader 1 is a protein-targeting chimera designed to selectively target and degrade the N-terminal domain of the Androgen Receptor (AR-V7). This small molecule exhibits significant efficacy in inducing apoptosis in prostate cancer cells, demonstrating a degradation efficiency of 62.2% at 1 μM and 71.1% at 5 μM in VCaP cells. PROTAC AR-NTD degrader 1 is a valuable tool for research focused on androgen receptor signaling and its implications in prostate cancer therapy. -
PROTAC IRAK4 Degrader
KT-474 hydrochloride is a potent PROTAC degrader targeting IRAK4, exhibiting significant anti-tumor properties. This compound inhibits the cell cycle and induces apoptosis in affected cells, demonstrating tumor regression in xenograft models of MYD88-mutated ABC DLBCL. Additionally, KT-474 features an alkyne group facilitating click chemistry, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it a valuable tool for chemical biology research. -
HDAC1-3 PROTAC Degrader
JPS004 is a targeted proteolysis targeting chimera (PROTAC) that degrades histone deacetylases HDAC1-3. By inducing the degradation of these enzymes, JPS004 facilitates histone acetylation, which can promote apoptosis in cancer cells. This compound is valuable for research into cancer biology and therapeutic strategies aimed at modulating epigenetic modifications. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-16 is an effective degrader specifically targeting BRD4, with IC50 values of 34.58 nM for BRD4 (BD1) and 40.23 nM for BRD4 (BD2). This compound is known to significantly reduce Cyclin B1 expression, which is associated with G2/M cell cycle progression. Additionally, PROTAC BRD4 Degrader-16 effectively induces apoptosis in MV-4-11 cells, contributing to its potential utility in cancer research and therapeutic applications. -
Bcr-AblT315 PROTAC Degrader
PROTAC BCR-ABL Degrader-2 is a selective degrader targeting the Bcr-AblT315 mutant, with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. This compound demonstrates a notable degradation efficacy, achieving degradation rates of 69.89% and 94.23% at concentrations of 100 nM and 300 nM, respectively. Additionally, it shows promising in vivo anti-tumor effects including significant tumor regression and induction of apoptosis in tumor cells, while maintaining a favorable safety profile. PROTAC BCR-ABL Degrader-2 is suitable for research focused on chronic myeloid leukemia (CML). -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 6 is a selective degrader targeting the EGFRDel19 mutant, exhibiting a DC50 value of 45.2 nM in HCC827 cells. This compound effectively induces apoptosis and leads to G1 phase cell cycle arrest in HCC827 cells. Its unique mechanism of action makes it a valuable tool for research focused on EGFR-related pathways and the development of targeted cancer therapies. -
PROTAC HDAC6 Degrader
PROTAC HDAC6 Degrader 1 is a selective compound designed to target and degrade histone deacetylase 6 (HDAC6) through the proteolysis-targeting chimera (PROTAC) mechanism. With a DC50 of 3.5 nM, this degrader exhibits significant antiproliferative effects, particularly by inducing apoptosis in myeloid leukemia cell lines. It serves as a valuable tool for research on cancer therapies and the modulation of histone deacetylation pathways. -
PROTAC c-Met Degrader
PROTAC c-Met Degrader-4 is a potent orally active PROTAC designed to target c-MET for degradation. It exhibits remarkable intracellular degradation potency with a DC50 value of less than 0.5 nM and effectively induces cell cycle arrest and apoptosis while inhibiting cell invasion and migration. This compound is particularly useful in cancer research, demonstrating the ability to suppress proliferation and inhibit the growth of various cancers, including non-small cell lung cancer and gastric cancer. In vivo studies also highlight its effectiveness in reducing tumor growth in Hs746T xenograft models.
