PROTACs
PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.
PROTACs Isoform Specific Products
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PROTACs Related Products (1390)
Related Products (1390)
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Antibodies (1)
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PROTACs Isoform Comparison
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(Rac)-P1D-34
0 Images(Rac)-P1D-34 is a Pin1 PROTAC degrader that recruits cereblon, with a DC50 of 177 nM. (Rac)-P1D-34 induces Pin1 degradation via proteasome- and ubiquitin-like modification-dependent pathways. (Rac)-P1D-34 upregulates ROS and DNA damage, downregulates the UPR pathway, and inhibits leukemia cell proliferation; it also sensitizes drug-resistant acute myeloid leukemia cells to Venetoclax (ABT-199) (HY-15531) by downregulating Mcl-1 levels. (Rac)-P1D-34 can be used in the research of acute myeloid leukemia.
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FC-14369
0 ImagesCat. No.: HY-171860CAS No.: 3066894-28-5FC-14369 is a PROTAC degrader targeting the HIV-1 Nef protein, with a DC50 value of 160 nM. Through its bifunctional structure, FC-14369 binds to Nef and the Cereblon E3 ubiquitin ligase, induces Nef ubiquitination and proteasomal degradation, restores the expression of cell-surface CD4 and MHC-I, and inhibits HIV-1 replication. FC-14369 can be used in research on HIV infection and AIDS. FC-14369 is applicable to studies related to HIV-1 infection.
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PROTAC Chk1 degrader-1
0 ImagesPROTAC Chk1 degrader-1 is a Chk1-targeting PROTAC.PROTAC Chk1 degrader-1 recruits the Cereblon E3 ligase to induce ubiquitination and proteasomal degradation of Chk1.PROTAC Chk1 degrader-1 exhibits Chk1 degradation activity in malignant melanoma cells without showing a hook effect.PROTAC Chk1 degrader-1 can be used for the research of malignant melanoma.
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PROTAC CDK2/4/6 Degrader-2
0 ImagesCat. No.: HY-185121CAS No.: 2541626-49-5PROTAC 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 (HY-171826) 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.
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LC-MF-4
0 ImagesCat. No.: HY-174981Purity: 98.46%LC-MF-4 is an orally active VHL-recruiting FGFR3 PROTAC degrader and hERG potassium channel inhibitor. LC-MF-4 has an IC50 of 16.6 nM against human FGFR3, exhibits inhibitory activity against hERG potassium channels, suppresses the expression of genes related to mitochondrial biogenesis and ATP synthesis, inhibits cancer cell proliferation, and shows significant antitumor activity in mice. LC-MF-4 can be used in the research of bladder cancer, urothelial carcinoma, FGFR3Y373C mutant cancers, and FGFR3-TACC3 fusion-positive cancers.
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PROTAC G9a/GLP degrader 1
0 ImagesCat. No.: HY-178065Purity: 98.22%PROTAC G9a/GLP degrader 1 is a PROTAC degrader targeting G9a/GLP histone methyltransferases, with DC50 values of 336 nM and 988 nM against G9a and GLP, respectively. PROTAC G9a/GLP degrader 1 reduces H3K9me2 levels, inhibits breast cancer cell migration, and has no effect on cell viability. PROTAC G9a/GLP degrader 1 can be used in breast cancer-related research.
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DDC-01-163
0 ImagesDDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer.
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Homo-BacPROTAC6
0 ImagesCat. No.: HY-153571Homo-BacPROTAC6 is a ClpC1NTD BacPROTAC degrader and can targets ClpC2. Homo-BacPROTAC7 efficiently kill M. tuberculosis.
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CG428-NEG
0 ImagesCat. No.: HY-157542CAS No.: 2714560-39-9CG428-NEG is the negative control of PROTAC CG428 (HY-137465). CG428-NEG binds to TRKA, TRKB and TRKC with high affinity, with Kd values of 0.88 nM, 4.8 nM and 59.8 nM, respectively. CG428-NEG inhibits the growth of cancer cells and reduces the level of TPM3-TRKA fusion protein in cancer cells. CG428-NEG can be used in the research of colorectal cancer.
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PROTAC AR Degrader-4 TFA
0 ImagesCat. No.: HY-111848APurity: 99.26%PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
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ML 2-14
0 ImagesCat. No.: HY-132991Purity: 99.43%ML 2-14 is a PROTAC targeting BRD4 with a C4 alkyl linker. ML 2-14 consists of the E3 ligase ligand EN219 (HY-115715) (bule part), the target protein ligand JQ-1 (HY-13030) (red part), and the PROTAC linker (balck part). ML 2-14 can effectively degrade BRD4 in 231MFP breast cancer cells, and this effect can be reversed by the proteasome inhibitor Bortezomib (HY-10227) and the E1 activase inhibitor TAK-243 (HY-100487). ML 2-14 can be used for breast cancer-related research.
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A947
0 ImagesCat. No.: HY-148381CAS No.: 2378056-80-3A947 is a VHL-based SMARCA2 PROTAC degrader with a DC50 of 39 pM and a Kd of 93 nM for human SMARCA2. A947 recruits SMARCA2 to the VHL E3 ubiquitin ligase for ubiquitination modification, mediates its degradation via the proteasome, and exerts selective degradation effects on SMARCA4 and PBRM1. A947 induces G1 cell cycle arrest, inhibits transcription, and exerts growth inhibitory effects in SMARCA4G12C-mutant cancer cells. A947 acts synergistically with MCL1 inhibitors to induce apoptosis in SMARCA4G12C-mutant cancer cells. A947 can be used in studies related to SMARCA4G12C-mutant non-small cell lung cancer and non-small cell lung cancer.
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(rel)-PROTAC ERRα Degrader-1
0 ImagesCat. No.: HY-128838APurity: 98.18%
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BTX-6654
0 ImagesCat. No.: HY-161233BTX-6654 is a SOS1 PROTAC degrader. BTX-6654 induces ubiquitination and degradation of SOS1 via the proteasomal pathway by bridging SOS1 with the E3 ligase CRBN to form a ternary complex, thereby blocking KRAS activation and downregulating the MAPK signaling pathway (pERK/pS6), and ultimately inhibiting tumor growth. BTX-6654 can be used in research on various cancers driven by KRAS mutations.
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PROTAC HPK1 Degrader-5
0 ImagesCat. No.: HY-175547CAS No.: 3108744-13-1PROTAC HPK1 Degrader-5 is an orally effective and selective HPK1 PROTAC degrader with a DC50 of 5.0 nM. PROTAC HPK1 Degrader-5 recruits the CRBN E3 ligase to specifically induce the degradation of HPK1 via the ubiquitin-proteasome system, which in turn significantly inhibits SLP76 phosphorylation and enhances the activation of the ERK pathway, thereby stimulating the release of IL-2 and IFN-γ. PROTAC HPK1 Degrader-5 can be used in studies related to tumor immunity (e.g., colorectal cancer).
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SJ45566
0 ImagesSJ45566 a potent and orally active PROTAC-based LCK degrader, with a DC50 of 1.21 nM. SJ45566 can be used in the research for T‑Cell Acute Lymphoblastic Leukemia.
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APH02174
0 ImagesAPH02174 is an orally effective and selective IRAK4 PROTAC degrader with a DC50 of 4.01 nM in THP-1 cells. APH02174 inhibits LPS (HY-D1056)-induced IL-6 release by degrading IRAK4 and blocking TLR/IL-1R downstream signaling. APH02174 exhibits favorable anti-inflammatory activity in both Imiquimod (HY-B0180)-induced psoriasis-like skin inflammation and collagen-induced arthritis models. APH02174 is useful for research on inflammatory diseases such as psoriasis and rheumatoid arthritis.
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PROTAC RNF4 degrader-1
0 ImagesCat. No.: HY-181692Purity: 98.09%PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (Kd = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. PROTAC RNF4 degrader-1 induces DNA damage, apoptosis, and exhibits antiproliferative activity in cancer cells. PROTAC RNF4 degrader-1 displays antitumor activity with no obvious side effects in mouse models. PROTAC RNF4 degrader-1 is applicable to the research of hepatocellular carcinoma.
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MS15
0 ImagesCat. No.: HY-151613CAS No.: 3035638-40-2
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PROTAC AR Degrader-4
0 ImagesCat. No.: HY-111848CAS No.: 1351169-31-7PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
