PROTAC
The PROTAC molecule itself contains three distinct portions: a ligand for binding to the target protein, a ligand for binding to an E3 ligase, and a linker joining these two ligands.
PROTACs (proteolysis-targeting chimaeras) are bifunctional molecules that bring a target protein into spatial proximity with an E3 ubiquitin ligase to trigger target ubiquitination and subsequent proteasomal degradation. Effective redirection of ligase poly-ubiquitination activity toward a new substrate protein requires formation of a ligase:PROTAC:target ternary complex, an intermediate species that is crucial to the cellular activity of degrader molecules. A characteristic feature of PROTACs mode of action is their sub-stoichiometric catalytic activity that alleviates the requirement for target engagement and occupancy of traditional inhibitors. New PROTAC molecules designed guided by the crystal structure show exquisite selectivity for inducing cellular depletion of Brd4 over its BET family members Brd2 and Brd3.
Targets for PROTAC
Products for PROTAC
- Cat.No. Product Name Information
- GC68352 (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
- GC33280 A1874 A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
- GC35227 ACBI1 ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis.
- GC32685 ARV-771 ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
- GC19038 ARV-825 ARV-825 is a BRD4 Inhibitor based on PROTAC technology.
- GC33354 AT6 AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 with highly selectivity to bromodomain (Brd4).
- GC64271 AU-15330 AU-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.
- GC65506 BETd-246 BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.
- GC32791 BETd-260 (ZBC 260) BETd-260 (ZBC 260) (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 (ZBC 260) potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
- GC65457 BI-3663 BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 linked to Pomalidomide with a linker. Anti-cancer activity.
- GC33017 BRD4 degrader AT1 BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4BD2 in cells.
- GC65128 BSJ-03-123 BSJ-03-123 is a PROTAC connected by ligands for Cereblon and CDK as a potent and novel CDK6-selective small-molecule degrader.
- GC67861 CCT367766 formic
- GC35635 CDK9 Antagonist-1
- GC35739 CP-10 CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6.
- GC66361 DB-0646 DB-0646, a PROTAC, is a multi-kinase degrader.
- GC19119 dBET1 dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
- GC35815 dBET57 dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4Cereblon E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2.
- GC32719 dBET6 dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity.
- GC35882 dMCL1-2 dMCL1-2 is a potent and selective PROTAC of myeloid cell leukemia 1 (MCL1) (Bcl-2 family member) based on Cereblon, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1.
- GC67914 dTAGV-1 TFA
- GC35904 dTRIM24 dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24.
- GC32902 E3 ligase Ligand-Linker Conjugates 10 E3 ligase Ligand-Linker Conjugates 10 (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. E3 ligase Ligand-Linker Conjugates 10 incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. E3 ligase Ligand-Linker Conjugates 10 is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
- GC32987 E3 ligase Ligand-Linker Conjugates 8 E3 ligase Ligand-Linker Conjugates 8 (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. E3 ligase Ligand-Linker Conjugates 8 incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. E3 ligase Ligand-Linker Conjugates 8 is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
- GC32976 E3 ligase Ligand-Linker Conjugates 9 E3 ligase Ligand-Linker Conjugates 9 is a conjugate of ligands for E3 and 25-atom-length linker. The connector of linker is Halogen group. E3 ligase Ligand-Linker Conjugates 9 incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. E3 ligase Ligand-Linker Conjugates 9 is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
- GC36001 ERD-308 ERD-308 is a highly potent von Hippel-Lindau-based PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).
- GC19509 Gefitinib-based PROTAC 3 A VHL-recruiting PROTAC
- GC36167 GMB-475 GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
- GC32831 HaloPROTAC 2 HaloPROTAC 2 (HaloPROTAC 2) is a conjugate of ligands for E3 and 21-atom-length linker. The connector of linker is Halogen group. HaloPROTAC 2 incorporates the VH032 based VHL ligand and 5-unit PEG linker. HaloPROTAC 2 is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
- GC33391 Homo-PROTAC cereblon degrader 1 Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.
- GC65285 Homo-PROTAC pVHL30 degrader 1 Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC, consists of two ligands of von Hippel-Lindau.
- GC65559 INY-03-041 INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide (Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.
- GC67757 INY-03-041 trihydrochloride
- GC65471 JH-XI-10-02 JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.
- GC38812 MD-224 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 consists of ligands for Cereblon and MDM2. 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.
- GC64651 MI-389 MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4CRBN E3 ligase.
-
GC69501
MS159
MS159 is an effective nuclear receptor binding SET domain protein 2 (NSD2) PROTAC degrader. MS159 can inhibit the growth of tumor cells. MS159 is an effective chemical tool for exploring the role of NSD2 in health and disease.
- GC65466 MS170 MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively.
- GC67710 MS177
-
GC69502
MS21
MS21 is a novel AKT degrader that selectively inhibits the growth of mutant cancers through the PI3K/PTEN pathway.
- GC65243 MS4077 MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 37?nM for binding affinity to ALK.
- GC64966 MS4078 MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19?nM for binding affinity to ALK.
- GC64292 MS432 MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
- GC65052 MS4322 MS4322 (YS43-22) is a first-in-class PRMT5 degrader and a valuable chemical tool (PROTAC) for exploring the PRMT5 functions in health and disease.
- GC65876 MS4322 (isomer) MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a potent and selective PRMT5 (protein arginine methyltransferase 5) degrader, and inhibits growth of multiple cancer cell lines.
- GC64295 MS67 MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.
-
GC69505
MS9427
MS9427 is an effective PROTAC EGFR degrader, with Kd values of 7.1 nM and 4.3 nM for wild-type EGFR and mutant EGFR L858R, respectively. MS9427 selectively degrades mutant variants through the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathway, but does not degrade WT EGFR. MS9427 has a strong inhibitory effect on NSCLC cell proliferation and can be used in cancer research.
-
GC69506
MS9427 TFA
MS9427 TFA is an effective PROTAC EGFR degrader, with Kd values of 7.1 nM and 4.3 nM for wild-type EGFR and mutant EGFR L858R, respectively. MS9427 TFA selectively degrades mutant variants through the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathway, but not WT EGFR. MS9427 TFA strongly inhibits NSCLC cell proliferation and can be used in cancer research.
- GC36661 MT-802 MT-802 is a potent BTK degrader based on Cereblon ligand, with a DC50 of 1 nM.
-
GC69744
MTX-23
MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cell proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis in cells.
- GC18729 MZ1 MZ1 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4).
- GC33102 MZP-54 MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 4 nM for Brd4BD2.
- GC33363 MZP-55 MZP-55 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 8 nM for Brd4BD2.
- GC67889 NJH-2-056
- GC64344 PhosTAC7 Similar to PROTACs in their ability to induce ternary complexes, PhosTAC7 focuses on recruiting a Ser/Thr phosphatase to a phosphosubstrate to mediate its dephosphorylation.
-
GC69730
PP-C8
PP-C8 is an effective selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces degradation of CDK12-Cyclin K with DC50 values of 416 and 412 nM, respectively. PP-C8 exhibits highly efficient synergistic anti-proliferative effects with PARP inhibitors in triple-negative breast cancer (TNBC).
- GC36981 PROTAC AR Degrader-4
- GC68376 PROTAC AR-V7 degrader-1
- GC65479 PROTAC B-Raf degrader 1 PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.
- GC38941 PROTAC Bcl2 degrader-1 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.
- GC33109 PROTAC BET Degrader-1 PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
- GC32980 PROTAC BET degrader-2 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.
- GC34325 PROTAC BET degrader-3 PROTAC BET Degrader-3 is a PROTAC connected by ligands for von Hippel-Lindau and BET.
- GC68289 PROTAC BRAF-V600E degrader-1
-
GC69745
PROTAC BRD4 Degrader-11
PROTAC BRD4 Degrader-11 (compound 9a) is an effective PROTAC that links von Hippel-Lindau ligand and BRD4 ligand. PROTAC BRD4 Degrader-11 can be coupled with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with DC50 values of 0.23 nM and 0.38 nM, respectively.
- GC64436 PROTAC BRD4 Degrader-9 PROTAC BRD4 Degrader-9 (compound 8a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-9 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.86 nM and 7.6 nM, respectively.
- GC33372 PROTAC BRD9 Degrader-1 PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.
-
GC69746
PROTAC BRD9 Degrader-4
PROTAC BRD9 Degrader-4 is a dual-function degrader of BRD9, which is being studied for cancer research.
-
GC69748
PROTAC CDK12/13 Degrader-1 TFA
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly efficient and selective dual degrader of cell cycle-dependent kinases CDK12/CDK13, with DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used for research on breast cancer.
- GC32845 PROTAC CDK9 Degrader-1 PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.
- GC34730 PROTAC CRABP-II Degrader-1 PROTAC CRABP-II Degrader-1 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand.
- GC34731 PROTAC CRABP-II Degrader-2 PROTAC CRABP-II Degrader-2 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand.
- GC34732 PROTAC CRABP-II Degrader-3 PROTAC CRABP-II Degrader-3 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand.
- GC36982 PROTAC CRBN Degrader-1 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.
-
GC69749
PROTAC CYP1B1 degrader-1
PROTAC CYP1B1 degrader-1 (Compound 6C) is an α-naphthoflavone derivative that can eliminate drug resistance mediated by cytochrome P450 (CYP)1B1 by targeting and degrading it. Its IC50 values for CYP1B1 and CYP1A2 are 95.1 and 9838.6 nM, respectively. PROTAC CYP1B1 Degrader-1 can be used to study prostate cancer with overexpression of CYP1B1.
- GC34733 PROTAC ER Degrader-2 PROTAC ER Degrader-2 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
- GC34734 PROTAC ER Degrader-3 PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
- GC64350 PROTAC ER Degrader-4 PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.
- GC34735 PROTAC ERα Degrader-2
- GC34341 PROTAC ERα Degrader-1 PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
- GC36983 PROTAC ERRalpha Degrader-1 PROTAC ERRalpha Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.
- GC36984 PROTAC ERRalpha Degrader-2 PROTAC ERRalpha Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader.
- GC65509 PROTAC EZH2 Degrader-1 PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes.
- GC36985 PROTAC FAK degrader 1 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.
- GC65555 PROTAC FLT-3 degrader 1 PROTAC FLT-3 degrader 1 is a von Hippel-Lindau-based PROTAC FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction.
- GC64825 PROTAC HSP90 degrader BP3 PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 ?M). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell.
-
GC69750
PROTAC IRAK3 degrade-1 formic
PROTAC IRAK3 degrade-1 (compound 23) formic acid is an effective and selective IRAK3 degrader (IC50 = 5 nM).
- GC38942 PROTAC K-Ras Degrader-1 PROTAC K-Ras Degrader-1 (Compound 518) is potent K-Ras degrader based on Cereblon E3 ligand, exhibits ≥70% degradation efficacy in SW1573 cells.
- GC63878 PROTAC KRAS G12C degrader-1 Mal-amido-PEG8-C2-acid (example 142) is a nonclaevable ADC linker, extracted from patent US2018339985.
- GC38943 PROTAC Mcl1 degrader-1 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 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity.
- GC37010 PROTAC MDM2 Degrader-1 PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC37011 PROTAC MDM2 Degrader-2 PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC37012 PROTAC MDM2 Degrader-3 PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC37013 PROTAC MDM2 Degrader-4 PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
- GC65147 PROTAC PARP1 degrader 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.
- GC34740 PROTAC RAR Degrader-1 PROTAC RAR Degrader-1 comprises a IAP ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
- GC33418 PROTAC Sirt2 Degrader-1 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).
- GC63916 PROTAC-O4I2 PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.
- GC33217 QCA570 QCA570 is a PROTAC connected by ligands for Cereblon and BET, with an IC50 of 10 nM for BRD4 BD1 Protein.
- GC65898 SB1-G-187 SB1-G-187, a PROTAC, is a multi-kinase degrader.