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 About 30 results found for searched term "PROTAC" (0.036 seconds)

Cat.No.  Name Target
M10379 BSJ-03-123 PROTAC
PROTAC CDK6 Degrader
BSJ-03-123 is a novel, potent CDK6-selective small-molecule degrader (PROTAC).
M10382 PROTAC SGK3 degrader-1 PROTAC
SGK3-PROTAC1
PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a potent SGK3 degrader, it is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3.
M10383 Homo-PROTAC cereblon degrader 1 (OUN20985) PROTAC
OUN20985
Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.
M10384 Homo-PROTAC pVHL30 degrader 1 PROTAC
CM11 VHL inhibitor
Homo-PROTAC pVHL30 degrader 1 is a pVHL30 degrader based on PROTAC and a potent VHL inhibitor.
M14871 Gefitinib-based PROTAC 3 PROTAC
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau 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.
M14873 PROTAC BET Degrader-1 PROTAC
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
M14874 PROTAC BET degrader-2 PROTAC
PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
M14875 PROTAC FAK degrader 1 PROTAC
PROTAC FAK degrader 1 is a selective and potent von Hippel-Lindau-based focal adhesion kinase (FAK) degrader with an IC50 of 6.5 nM, DC50 of 3 nM.
M21231 PROTAC CDK9 Degrader-1 PROTAC
PROTAC CDK9 Degrader-1 is a PROTAC linked by Cereblon ligand and CDK ligand and is a selective CDK9 degrader.
M25473 HaloPROTAC3 Ligand for E3 Ligase
VH285-PEG4-C4-Cl
HaloPROTAC3 is a conjugate of ligands for E3 and 16-atom-length linker, and it is also a highly potent and efficacious degrader of GFP-HaloTag7 fusion proteins with a DC50 of 19 nM.
M28222 PROTAC AR Degrader-4  PROTAC
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).
M28867 VH032-PEG5-C6-Cl PROTAC
HaloPROTAC 2
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a conjugate of ligands for E3 and 21-atom-length linker. The connector of linker is Halogen group. VH032-PEG5-C6-Cl incorporates the VH032 based VHL ligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
M28878 PROTAC RIPK degrader-2  PROTAC
PROTAC RIPK degrader-2 is a nonpeptidic PROTAC based on von Hippel-Lindau ligand which potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.
M29136 PROTAC TBK1 degrader-2  PROTAC
PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM).
M29153 FKBP12 PROTAC dTAG-7 PROTAC
dTAG-7
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
M29154 FKBP12 PROTAC dTAG-13 PROTAC
dTAG-13
FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12F36V and CRBN, thereby selectively degrading FKBP12F36V.
M29225 PROTAC Sirt2 Degrader-1  Sirtuin
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM).
M29314 PROTAC Mcl1 degrader-1  PROTAC
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM.
M29496 PROTAC ERRα Degrader-1  PROTAC
PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.
M29501 PROTAC BRD4 Degrader-3  PROTAC
PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC connected by ligands for von Hippel-Lindau and BRD4.
M29528 PROTAC CRBN Degrader-1  PROTAC
PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader.
M29530 PROTAC IRAK4 degrader-1  PROTAC
PROTAC IRAK4 degrader-1 is a Cereblon-based PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively.
M29542 HaloPROTAC-E  SGK
HaloPROTAC-E is a novel HaloPROTAC potent degrader, inducing reversible degradation of two endosomally localized proteins, SGK3 and VPS34, with a DC50 of 3-10 nM, remarkably selective inducing only degradation of the Halo tagged endogenous VPS34 complex (VPS34, VPS15, Beclin1, and ATG14).
M29548 PROTAC PARP1 degrader  PROTAC
PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
M29577 PROTAC Bcl2 degrader-1  PROTAC
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.
M29635 PROTAC IRAK4 degrader-7  PROTAC
KT-474; SAR444656
PROTAC IRAK4 degrader-7 (Compound I-417) is a potentially first-in-class, orally active PROTAC IRAK4 degrader with antitumor activity for studies related to hidradenitis suppurativa (HS) and atopic dermatitis (AD).
M29649 PROTAC PD-1/PD-L1 degrader-1  PROTAC
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
M29813 PROTAC STING Degrader-1  STING
PROTAC STING Degrader-1 (Compound SP23) is a STING PROTAC degrader with a DC50 of 3.2 μM. PROTAC STING Degrader-1 shwos anti-inflammatory activity.
M31078 PROTAC AR Degrader-4 TFA  PROTAC
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).
M31276 PROTAC CDK2/9 Degrader-1  PROTAC
PROTAC CDK2/9 Degrader-1 is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand.



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