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| Cat. No. | Product Name | Field of Application | Chemical Structure |
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| DC81377 | PROTAC HDAC3 degrader-1 |
PROTAC HDAC3 degrader-1 is a selective PROTAC degrader targeting HDAC3 with a DC50 of 30.73 nM. PROTAC HDAC3 degrader-1 induces degradation of HDAC3 via the ubiquitin-proteasome system. PROTAC HDAC3 degrader-1 promotes apoptosis, induces DNA damage, and downregulates anti-apoptotic proteins Mcl-1 and Bcl-xL. PROTAC HDAC3 degrader-1 can be used for the research of acute myeloid leukemia.
(Pink: HDAC3 ligand ; Blue: VHL ligand ; Black: linker).
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| DC81376 | PROTAC hCAII degrader-1 |
PROTAC hCAII degrader-1 is a potent PROTAC human carbonic anhydrase II (hCAII) degrader with an DC50 of 0.5 nM in HEK293 cells. PROTAC hCAII degrader-1 recruits cereblon (CRBN) E3 ubiquitin ligase to form a ternary complex. PROTAC hCAII degrader-1 enables ubiquitination and subsequent proteasomal degradation of hCAII.
(Pink: CA Ⅱ ligand ; Blue: Cereblon ligand ; Black: linker).
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| DC81375 | PROTAC GPX4 degrader-5 |
PROTAC GPX4 degrader-5 (compound N15) is an efficient and highly selective PROTAC GPX4 degrader (DC50 = 28 nM). PROTAC GPX4 degrader-5 can induce ferroptosis and has low toxicity to normal cells. PROTAC GPX4 degrader-5 can significantly increase ROS. PROTAC GPX4 degrader-5 exerts anti proliferative effects on various tumor cells. PROTAC GPX4 degrader-5 is commonly used in cancer research.
(Pink: GPX4 ligand ; Blue: Others ligand ; Black: linker ).
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| DC81372 | PROTAC EZH2 Degrader-45 |
PROTAC EZH2 Degrader-45 (compound 61) is a PROTAC protein degrader targeting EZH2 with an IC50 of 22.97 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-45 can be used for the research of diffuse large b-cell lymphoma.
(Pink: Histone Methyltransferase ligand ; Blue: VHL ligand ; Black: linker).
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| DC81371 | PROTAC EZH2 Degrader-44 |
PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer.
(Pink: EZH2 ligand ; Blue: VHL ligand ; Black: linker).
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| DC81370 | PROTAC EZH2 Degrader-43 |
PROTAC EZH2 Degrader-43 (compound 59) is a PROTAC protein degrader targeting EZH2 with an IC50 of 21.73 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-43 can be used for the research of lymphoma.
(Pink: Histone Methyltransferase ligand ; Blue: VHL ligand ; Black: linker).
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| DC81369 | PROTAC EZH2 Degrader-42 |
PROTAC EZH2 Degrader-42 (compound 57) is an EZH2-targeting PROTAC degrader and antiproliferative agent. PROTAC EZH2 Degrader-42 induces cIAP-mediated ubiquitination and subsequent proteasomal degradation of EZH2. PROTAC EZH2 Degrader-42 can be used for the research of lymphoma.
(Pink: Histone Methyltransferase ligand ; Blue: Aminopeptidase ligand ; Black: linker).
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| DC81368 | PROTAC EZH2 Degrader-41 |
PROTAC EZH2 Degrader-41 is an EZH2-targeting PROTAC and cIAP E3 ubiquitin ligase recruiter. PROTAC EZH2 Degrader-41 induces EZH2 degradation via ubiquitination and proteasomal breakdown. PROTAC EZH2 Degrader-41 exerts antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 can be used for the research of lymphoma.
(Pink: Histone Methyltransferase ligand ; Blue: cIAP ligand ; Black: ).
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| DC81367 | PROTAC EZH2 Degrader-40 |
PROTAC EZH2 Degrader-40 (compound 56) is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.35 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-40 can be used for the research of diffuse large B-cell lymphoma.
(Pink: Histone Methyltransferase ligand ; Blue: Aminopeptidase ligand ; Black: linker).
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| DC81364 | PROTAC EZH2 Degrader-31 |
PROTAC EZH2 Degrader-31(compound 69) is a PROTAC protein degrader targeting EZH2, with antiproliferative IC50 values of 3.63 μM in lSU-DHL-6 cells and 8.74 μM in HBL-1 cells. PROTAC EZH2 Degrader-31 can be used for the research of lymphoma.
(Pink: EZH2 ligand ; Blue: MDM2 ligand ; Black: linker).
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| DC81363 | PROTAC EZH2 Degrader-30 |
PROTAC EZH2 Degrader-30 (compound 67) is ais a PROTAC protein degrader targeting EZH2 with an IC50 of 6.22 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-30 can be used for the research of diffuse large B-cell lymphoma.
(Pink: EZH2 ligand ; Blue: MDM2 ligand ; Black: linker).
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| DC81362 | PROTAC EZH2 Degrader-29 |
PROTAC EZH2 Degrader-29 (compound 66) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 24.53 μM against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-29 can be used in studies related to diffuse large B-cell lymphoma.
(Pink: EZH2 ligand ; Blue: MDM2 ligand ; Black: linker).
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| DC81356 | PROTAC EZH2 Degrader-19 |
PROTAC EZH2 Degrader-19 (compound 6) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.00 nM. PROTAC EZH2 Degrader-19 induces strong degradation of all PRC2 subunits (EZH2, SUZ12, EED, RbAp48) in a concentration- and time-dependent manner.PROTAC EZH2 Degrader-19 exhibits antiproliferative effects in cancer cells.PROTAC EZH2 Degrader-19 can be used for the research of cancer.
(Pink: EZH2 ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).
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| DC81355 | PROTAC EZH2 Degrader-17 |
PROTAC EZH2 Degrader-17 (compound 52) is a PROTAC protein degrader targeting EZH2 with an antiproliferative IC50 of 18.32 μM in lymphoma cells. PROTAC EZH2 Degrader-17 exhibits antiproliferative activity against lymphoma cells. PROTAC EZH2 Degrader-17 can be used for the research of lymphoma.
(Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: linker).
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| DC81354 | PROTAC EZH2 Degrader-16 |
PROTAC EZH2 Degrader-16 (compound 51) is a PROTAC protein degrader targeting EZH2 with an IC50 of 13.74 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-16 exerts antiproliferative activity against diffuse large B-cell lymphoma cells. PROTAC EZH2 Degrader-16 can be used for the research of diffuse large B-cell lymphoma.
(Pink: Histone Methyltransferase ligand ; Blue: Cereblon ligand ; Black: linker).
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| DC81352 | PROTAC EZH2 Degrader-14 |
PROTAC EZH2 Degrader-14 is an EZH2 PROTAC degrader, with an IC50 of 18.21 μM against diffuse large B-cell lymphoma cells, and exhibits no antiproliferative activity against non-target cells at concentrations up to 30.00 μM. PROTAC EZH2 Degrader-14 can be used in studies related to diffuse large B-cell lymphoma.
(Pink: Histone Methyltransferase ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).
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| DC81350 | PROTAC EML4-ALK Degrader-2 |
PROTAC EML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to ALK with an IC50 of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research.
(Pink: EML4-ALK ligand ; Blue: Cereblon ligand ; Black: linker ).
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| DC81349 | PROTAC EGFR degrader 17 |
PROTAC EGFR degrader 17 (Compound 35) is an EGFR PROTAC degrader with a DC50 value of 0.49 nM. PROTAC EGFR degrader 17 promotes the ubiquitination and degradation of EGFR. PROTAC EGFR degrader 17 can be used in research on various cancers, including non-small cell lung cancer.
(Pink: EGFR ligand ; Blue: TNF Receptor ligand ; Black: linker).
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| DC81348 | PROTAC EGFR degrader 16 |
PROTAC EGFR degrader 16 (Compound 98) a selective EGFR PROTAC degrader with DC50 values of < 50 nM in NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R) and NCI-H1976 + CS (EGFR L858R-T970M-L797S). PROTAC EGFR degrader 16 can be used for the study of EGFR-driven cancerssuch as non-small cell lung cancer (Pink: EGFR ligand; Blue: CRBN ligand; Black: Linker; EGFR ligand + Linker).
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| DC81347 | PROTAC DAPK1 Degrader-1 |
PROTAC DAPK1 Degrader-1 (Compound CP1) is a DAPK1 PROTAC degrader with a DC50 of 119.6 nM. PROTAC DAPK1 Degrader-1 significantly increased the MDM2 protein level. PROTAC DAPK1 Degrader-1 significantly reduced the levels of cleaved caspase-3 and cleaved PARP in a cell apoptosis model induced by the neurotoxin ceramide, indicating that it effectively inhibits neuronal apoptosis by degrading DAPK1. PROTAC DAPK1 Degrader-1 can be used to study neurological diseases such as cerebral ischemia and traumatic brain injury (pink: DAPK1 ligand; blue: CRBN ligand; black: linker).
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| DC81345 | PROTAC CDK9 degrader-12 |
PROTAC CDK9 degrader-12 is a selective CDK9 PROTAC degrader with a DC50 of 23 nM. PROTAC CDK9 degrader-12 induces proteasome-dependent degradation of CDK9, blocks CDK9-mediated HIV-1 transcriptional elongation, and reduces HIV-1 RNA synthesis. PROTAC CDK9 degrader-12 is applicable to research related to HIV-1 infection.
(Pink: CDK9 ligand ; Blue: VHL ligand ; Black: linker).
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| DC81343 | PROTAC CDK2-pRb degrader-1 |
PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer).
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| DC81342 | PROTAC CDK2/4/6 Degrader-2 |
PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research.
(Pink: CDK2 and CDK4 and CDK6 ligand ; Blue: Cereblon ligand ; Black: linker).
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| DC81341 | PROTAC CDK2/4/6 Degrader-1 |
PROTAC CDK2/4/6 Degrader-1 is an orally active CDK2/CDK4/CDK6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-1 is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-1 can be used for malignant melanoma research.
(Pink: Aurora A ligand ; Blue: Cereblon ligand ; Black: linker).
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| DC81340 | PROTAC CBP/p300/BRD4 Degrader-1 |
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer.
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| DC81339 | PROTAC BTK Degrader-4 |
PROTAC BTK Degrader-4 (compound 15) is a potent PROTAC Bruton's tyrosine kinases (BTK) degrader (DC50 < 100 nM) with little immunomodulatory imide drug (IMiD) activity (DC50 = 0.345 μM, Dmax = 27.4%). PROTAC BTK Degrader-4 can be used for cancers, autoimmune diseases, and inflammatory diseases that are mediated by BTK.
(Pink: Btk ligand ; Blue: Ligands for E3 Ligase and Cereblon E3 ligase ligand; Black: linker).
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| DC81338 | PROTAC BTK degrader-14 |
PROTAC BTK degrader-14 (compound 112) is a PROTAC protein degrader targeting BTK. PROTAC BTK degrader-14 can be used for the research of cancer.
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| DC81332 | PROTAC AURKA degrader 2 |
PROTAC AURKA degrader 2 (compound D) is a potent and selective PROTAC AURKA degrader with an IC50 of 3.58 nM. PROTAC AURKA degrader 2 exhibits 21.6-fold selectivity for AURKA over AURKB (IC50 = 77.2 nM). PROTAC AURKA degrader 2 specifically depletes AURKA on the mitotic spindle.
(Pink: Aurora Kinase and Aurora A ligand ; Blue: Ligands for E3 Ligase and Cereblon ligand ; Black: linker ).
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| DC81331 | PROTAC ALK degrader-5 |
PROTAC ALK degrader-5 (Compound 17) is an efficient ALK PROTAC degrader, with its inhibitory effects on EML4-ALK and NPM-ALK being 27.4 nM and 116.5 nM respectively. PROTAC ALK degrader-5 exhibits potent anti-proliferative activity against H3122 and Karpas 299. PROTAC ALK degrader-5 effectively inhibits the phosphorylation of ALK and STAT3. PROTAC ALK degrader-5 can be used for the study of ALK-driven malignant tumors, such as human non-small cell lung cancer and anaplastic large cell lymphoma.
(Pink: Anaplastic lymphoma kinase (ALK) Target protein ligand; Blue: Cereblon ligand ; Black: linker).
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| DC81329 | PROTAC AAK1 Degard-1 |
PROTAC AAK1 Degard-1 (the fourth product on page 96) is an effective PROTAC AAK1 degrader that can be used in cancer research.
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