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 Produits associés (1320)
Produits associés (1320)
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Anticorps (1)
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PROTACs Isoform Comparison
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FKBP12 PROTAC dTAG-13
0 ImagesSynonyms: dTAG-13FKBP12 PROTAC dTAG-13 (dTAG-13) is a FKBP12F36V PROTAC degrader and a PXR partial agonist. FKBP12 PROTAC dTAG-13 induces ubiquitination and proteasomal degradation of proteins tagged with FKBP12F36V, without degrading wild-type FKBP12 or un-fused PXR. It weakly promotes the recruitment of SRC-1, strongly inhibits the interaction between NCoR and PXR, and upregulates the expression of CYP3A4 and other drug metabolism-related genes. FKBP12 PROTAC dTAG-13 is applicable to research related to breast cancer and leukemia[1].
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Bavdegalutamide
0 ImagesSynonyms: ARV-110Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer (Pink: AR ligand (HY-168299); Blue: E3 ligase ligand (HY-W093272); Black: linker (HY-W091986)).
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dTAGV-1 TFA
0 ImagesdTAGV-1 TFA is a selective FKBP12F36V PORTAC degrader. dTAGV-1 TFA induces rapid degradation of FKBP12F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 TFA is applicable to functional validation studies of cancer and undegradable oncoproteins.
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BSJ-05-037
0 ImagesBSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines. BSJ-05-037 blocks the activation of the NF-κB/GATA-3 signaling pathway, inhibits PLCγ1 phosphorylation, and reduces the proliferative capacity of T-cell lymphoma cells. BSJ-05-037 enhances the sensitivity of T-cell lymphoma cells to chemotherapy. In mouse models of T-cell lymphoma, BSJ-05-037 induces ITK degradation, reduces GATA-3 expression, decreases tumor volume, and reverses chemotherapy resistance. BSJ-05-037 is applicable to research related to T-cell lymphoma.
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CCT400028
0 ImagesCat. No.: HY-181311Pureté: 98.03%CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The KD values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC50 against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma.
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LD-110 triTFA
0 ImagesCat. No.: HY-178825APureté: 99.56%LD-110 triTFA is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 triTFA promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 triTFA inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 triTFA can be used for the study of esophagus squamous cancer.
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DT2216
0 ImagesDT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
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AU-15330
0 ImagesAU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.
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Vepdegestrant
0 ImagesSynonyms: ARV-471Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
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Luxdegalutamide
0 ImagesSynonyms: ARV-766; JSB462Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer.
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AK-1690
0 ImagesAK-1690 is a selective PROTAC degrader targeting STAT6 (DC50=1 nM) with a Ki of 6 nM against human STAT6. AK-1690 degrades STAT6 via the interaction of STAT6 with cereblon and a ubiquitin-like process. AK-1690 effectively depletes STAT6 protein in mouse liver and lung tissues, and is applicable to research related to leukemia, Hodgkin's lymphoma, follicular lymphoma, etc..
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BMS-986365
0 ImagesSynonyms: CC-94676BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC).
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SD-36
0 ImagesCat. No.: HY-129602CAS No.: 2429877-44-9SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase. SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
