2116
Cat No. | Product Name | Synonyms | Targets |
---|---|---|---|
T4495 | DBET1 | Epigenetic Reader Domain | |
dBET1 is a hybrid molecule that combines (+)-JQ1 and thalidomide. It induces cereblon-dependent BET protein degradation in vitro (EC50: 430 nM) and induces apoptosis. | |||
T5440 | Dbet57 | Epigenetic Reader Domain | |
dBET57 is heterobifunctional degrader of BRD4 based on the PROTAC technology, exhibits significant degradation of BRD4BD1 with a DC50/5h of 500 nM ,and inactive on BRD4BD2 | |||
T5395 | BSJ-03-123 | CDK | |
BSJ-03-123 is a potent, CDK6-selective small-molecule degrader. | |||
T5130 | DBET6 | Apoptosis , Epigenetic Reader Domain | |
dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity. | |||
T5442 | A1874 | Epigenetic Reader Domain , PROTACs | |
A1874 is a nutlin-based and BRD4-degrading PROTAC which induces BRD4 degradation in cells. Effective in inhibiting many cancer cell lines proliferation. | |||
T5435 | ARV-771 | Epigenetic Reader Domain | |
ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34, 4.7, 8.3, 7.6, 9.6, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively[1]. | |||
T5434 | ARV-825 | Epigenetic Reader Domain | |
ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested. | |||
T16157 | MT-802 | BTK , PROTACs | |
MT-802 is an effective BTK degrader based on PROTAC technology (DC50: 1 nM). MT-802 has the potential to treat C481S mutant chronic lymphocytic leukemia (CLL). | |||
T18787 | TD-165 | Others , Ligand for E3 Ligase | |
TD-165, a PROTAC-based cereblon (CRBN) degrader, consists of a cereblon (CRBN) ligand-binding group, a linker, and a von Hippel-Landau (VHL) binding group[1]. | |||
T8488 | GMB-475 | Bcr-Abl | |
GMB-475 is a BCR-ABL1 tyrosine kinase degrader 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 ubiquitinati... | |||
T17350 | ACBI1 | Apoptosis , Epigenetic Reader Domain , PROTACs | |
ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in ... | |||
T17069 | THAL-SNS-032 | CDK | |
THAL-SNS-032 is a selective CDK9 degrader PROTAC. | |||
T13954 | UNC6852 | Histone Methyltransferase , Ligands for Target Protein for PROTAC | |
UNC6852 contains an EED ligand (IC50 = 247 nM) and a von Hippel-Lindau ligand and is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC. | |||
T9370 | DCBP-1 | Epigenetic Reader Domain , Ligand for E3 Ligase | |
dCBP-1 is a chemical degrader of p300/CBP. dCBP-1 hijacks the E3 ubiquitin ligase CRBN for selective degradation of p300/CBP. Degradation of p300/CBP by dCBP-1 leads to effective multiple myeloma cell killing. | |||
T36694 | XY028-140 | XY028-140 | CDK , Ligand for E3 Ligase |
XY028-140 is a selective CDK4/CDK6 degrade and inhibits both CDK4/6 expression and activity in cancer cells. XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. | |||
T9117 | BSJ-4-116 | CDK , Ligand for E3 Ligase | |
BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). | |||
T5436 | MZ 1 | Epigenetic Reader Domain | |
MZ 1 is a BRD4 protein degrader based on PROTAC technology. | |||
T39695 | ARD-2128 | Androgen Receptor | |
ARD-2128 is a highly potent, orally bioavailable PROTAC (proteolysis-targeting chimera) degrader of the androgen receptor (AR), effectively diminishing AR protein levels, suppressing AR-regulated gene expression in tumor... | |||
T13721 | Homo-PROTAC cereblon degrader 1 | Others , Ligand for E3 Ligase | |
Homo-PROTAC cereblon degrader 1 is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3. | |||
T13722 | Homo-PROTAC pVHL30 degrader 1 | Others , Ligand for E3 Ligase | |
Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC. | |||
T5437 | Gefitinib-based PROTAC 3 | EGFR | |
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, respectivel... | |||
T16153 | MS4078 | ALK , Ligand for E3 Ligase | |
MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK. | |||
T8745 | PROTAC BRAF-V600E degrader-1 | Compound 23 | Raf |
PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF. | |||
T39710 | ARV-471 | Vepdegestrant | Estrogen Receptor/ERR |
ARV-471 (Vepdegestrant) is a orally active Cereblon -based estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer. | |||
T11980 | MD-224 | Mdm2 , E1/E2/E3 Enzyme , PROTACs | |
MD-224 is a highly potent and efficacious MDM2 degrader based on the proteolysistargeting chimera (PROTAC) concept,and as a new class of anticancer agent. | |||
T5439 | BRD4 degrader AT1 | Epigenetic Reader Domain | |
BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells. | |||
T5438 | PROTAC CDK9 Degrader-1 | CDK | |
PROTAC CDK9 Degrader-1 is a selective CDK9 degrader. | |||
T18794 | Tetrazine-Ph-NHCO-C3-NHS ester | Others , PROTAC Linker | |
Tetrazine-Ph-NHCO-C3-NHS ester is a PEG-derived linker for PROTACs synthesis. | |||
T15203 | EGNHS | EGS crosslinker | Others |
EGNHS (EGS crosslinker) is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1]. | |||
T18566 | Propargyl-PEG12-bromide | Others , PROTAC Linker | |
Propargyl-PEG12-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. | |||
T18568 | Propargyl-PEG11-methane | Others , PROTAC Linker | |
Propargyl-PEG11-methane is a PEG-based PROTAC linker that can be used to synthesize PROTACs[1]. | |||
T39268 | Azido-PEG4-azide | Azido-PEG4-azide | PROTAC Linker |
Azido-PEG4-azide is a PEG-based PROTAC linker that can be used to synthesize PROTACs. | |||
T15839 | M-PEG12-amine | Others | |
m-PEG12-amine is a PEG-based PROTAC linker and a non-cleavable 12 unit PEG ADC linker employed in the synthesis of PROTACs[1] and antibody-drug conjugates (ADCs)[2]. | |||
T14250 | Amino-PEG8-amine | Others | |
Amino-PEG8-amine is a pegylated based PROTAC linker that can be used in the synthesis of PROTACs. It is a conjugate PEG derivative containing two amino (NH2) groups. | |||
T14450 | Azido-PEG4-hydrazide | Others | |
Azido-PEG4-hydrazide is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome sys... | |||
T18031 | Hydroxy-PEG10-acid | HO-PEG10-CH2CH2COOH | Others , PROTAC Linker |
Hydroxy-PEG10-acid (HO-PEG10-CH2CH2COOH) is a PEG-based PROTAC linker that can be used to synthesize PROTACs[1]. | |||
T38543 | 5-(Biotinamido)pentylamine | PROTAC Linker | |
5-(Biotinamido)pentylamine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. | |||
T18171 | M-PEG24-NH2 | Others , PROTAC Linker | |
m-PEG24-NH2 is a PEG-based PROTAC linker. m-PEG24-NH2 can be used in the synthesis of PROTACs. | |||
T18215 | M-PEG7-Br | Others , PROTAC Linker | |
m-PEG7-Br is a PEG-based PROTAC linker. m-PEG7-Br can be used in the synthesis of PROTACs. | |||
T18151 | M-PEG16-alcohol | Others , PROTAC Linker | |
m-PEG16-alcohol is a PEG-based PROTAC linker. m-PEG16-alcohol can be used in the synthesis of PROTACs. | |||
T18132 | M-PEG12-acid | Others , PROTAC Linker | |
m-PEG12-acid is a PEG-based PROTAC linker. m-PEG12-acid can be used in the synthesis of PROTACs. | |||
T18009 | HO-PEG13-OH | Others , PROTAC Linker | |
HO-PEG13-OH is a PEG-based PROTAC linker. HO-PEG13-OH can be used in the synthesis of PROTACs. | |||
T18222 | M-PEG8-O-alkyne | Others , PROTAC Linker | |
m-PEG8-O-alkyne is a PEG-based PROTAC linker. m-PEG8-O-alkyne can be used in the synthesis of PROTACs. | |||
T17964 | Fmoc-NH-PEG10-acid | Others , PROTAC Linker | |
Fmoc-NH-PEG10-acid is a PEG-based PROTAC linker. Fmoc-NH-PEG10-acid can be used in the synthesis of PROTACs. | |||
T18788 | Tert-Butyl 11-aminoundecanoate | PROTAC Linker | |
tert-Butyl 11-aminoundecanoate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. | |||
T18226 | M-PEG9-CH2COOH | Others , PROTAC Linker | |
m-PEG9-CH2COOH is a PEG-based PROTAC linker. m-PEG9-CH2COOH can be used in the synthesis of PROTACs. | |||
T18153 | M-PEG16-Br | Others , PROTAC Linker | |
m-PEG16-Br is a PEG-based PROTAC linker. m-PEG16-Br can be used in the synthesis of PROTACs. | |||
T18161 | M-PEG2-Br | Others , PROTAC Linker | |
m-PEG2-Br is a PEG-based PROTAC linker. m-PEG2-Br can be used in the synthesis of PROTACs. | |||
T18202 | M-PEG4-SH | Others , PROTAC Linker | |
m-PEG4-SH is a PEG-based PROTAC linker. m-PEG4-SH can be used in the synthesis of PROTACs. | |||
T18125 | M-PEG11-Br | Others , PROTAC Linker | |
m-PEG11-Br is a PEG-based PROTAC linker. m-PEG11-Br can be used in the synthesis of PROTACs. |