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PROTAC

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Cat. No. Product Name Field of Application Chemical Structure
DC11564 CDK9-PROTAC A heterobifunctional small molecule PROTAC capable of cereblon mediated proteasomal degradation of CDK9.
DC11590 Homo-PROTAC pVHL30 degrader 1 Featured CM-11 is a homo-PROTAC, bivalent small-molecule dimerizer of the VHL E3 ubiquitin ligase to induce self-degradation.
DC11867 TBK1 PROTAC 1 A novel potent, selective TBK1 PROTAC with DC50 of 12 nM, selectively degrades TBK1 with excellent selectivity against a related kinase IKKε.
DC11562 Sirt2-PROTAC-1 A novel SirReal-based PROTAC that induces isotype-selective Sirt2 degradation (IC50=0.25 uM)..
DC12702 A1874 Featured A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells).
DC10334 ARV-771 Featured ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader with Kd values of 4.7, 7.6, 7.6 nM against bromodomain 2, 3 and 4, respectively.
DC12024 ARV-825 Featured ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
DC11566 BETd-260 Featured BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.
DC11567 BETd-260 trifluoroacetate BETd-260 trifluoroacetate (ZBC260, BETd 260 TFA) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.
DC10997 BRD4 degrader AT1 BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
DC12380 BSJ-03-123 Featured BSJ-03-123 is a potent, CDK6-selective small-molecule degrader (PROTAC) that uniquely enables rapid pharmacological interrogation of CDK6-dependent functions.
DC11065 BTK PROTAC 10 BTK PROTAC 10 is a novel potent PROTAC for BTK with DC50 of 1.1 nM in cultured Ramos cells.
DC11064 BTK PROTAC 9 BTK PROTAC 9 is a novel potent PROTAC for BTK with DC50 of 5.9 nM in cultured Ramos cells, requires simultaneous engagement of BTK and CRBN to effectively degrade BTK.
DC11679 CCT-367766 Featured CCT367766 is a potent and the third generation heterobifunctional and PROTAC-based pirin targeting protein degradation probe (PDP), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein[1].
DC12023 dBET1 Featured dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
DC21893 dBET57 Featured dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2..
DC12022 dBET6 Featured dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM, and has antitumor activity.
DC11589 dBRD9 Featured dBRD9 is a PROTAC that bridge the BRD9 bromodomain and the cereblon E3 ubiquitin ligase complex.
DC20367 dTRIM24 Featured dTRIM24 is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement).
DC10932 HDAC6 degrader 9c HDAC6 degrader 9c (dHDAC6 9c) is a bifunctional molecule (dHDAC6) that could selectively degrade HDAC6, by conjugating non-selective HDAC inhibitor to a thalidomide-type E3 ligase ligand.
DC21351 MS4078 Featured MS4078 is a novel PROTAC (degrader) of ALK, potently decreases cellular levels of oncogenic active ALK fusion proteins in a concentration- and time-dependent manner in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells (DC50=11 nM).
DC21360 MZ1 Featured MZ1 is a PROTAC that tethers JQ1 to a ligand for the E3 ubiquitin ligase VHL, triggers, induces degradation of the BET bromodomain BRD4.
DC11040 QCA570 QCA570 is a novel, highly potent efficacious BET degrader (PROTAC).
DC11816 RapaLink-1 Featured RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors; blocks mTOR signaling of the F2108L mTOR and M2327I mTOR drug resistant mutants; RapaLink-1 is more potent mTOR inhibitor than rapamycin.
DC11584 SNIPER(ABL)-062 SNIPER(ABL)-062 is a novel, potent SNIPER molecule that tethers BCR-ABL inhibitor to a ligand of IAP, causes potent BCR-ABL degradation.
DC11749 THAL-SNS-032 Featured THAL-SNS-032 is a novel CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
DC11002 NTN21277(Gefitinib-based PROTAC 3) Featured Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.
DC11001 Foretinib-Based PROTAC 7
DC26169 MS1943 Featured MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines.
DC28018 MD-224 Featured MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.

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