protac pd 1/pd l1 degrader 1

PROTAC PD-1/PD-L1 degrader-1 is a PD-L1 degrading PROTAC that inhibits PD-1/PD-L1 interaction (IC50: 39.2 nM). PROTAC PD-1/PD-L1 degrader-1 restores immunity in Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model of suppressed immunity, which reduces the protein content of PD-L1 in a lysosomal-dependent manner.

(+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1/2) (IC50=77/33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

SMARCA-BD ligand 1 for Protac is a compound capable of binding to SMARCA2, the BAF ATPase subunit, based on the Protac technology for degrading SMARCA2

PROTAC BRD4 ligand-1 is a ligand for PROTAC GNE-987 targeting the BRD4 protein and is an inhibitor of BET.

Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

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.

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

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)[1].

PROTAC eDHFR Degrader-1 is a potent degrader targeting eDHFR-YFP and various proteins of interest (POIs), such as YFP and Luciferase [1].

PROTAC BRD9 Degrader-2 is a bifunctional compound designed for the targeted degradation of BRD9 in cancer research applications.

Cereblon inhibitor 1, an isoindoline derivative, serves as a modulator of the cereblon E3 ubiquitin ligase and shows promise for applications in cancer research.

PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.

1-Isothiocyanato-PEG3-azide is a PEG-based PROTAC linker utilized for PROTAC synthesis[1].

PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader.

U7D-1, a groundbreaking and selective ubiquitin-specific protease 7 (USP7) PROTAC degrader, exhibits a DC50 value of 33 nM in RS4;11 cells, demonstrating its potent anticancer properties. Furthermore, U7D-1 effectively induces apoptosis in Jeko-1 cells [1].

PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins (IC50 of 9.6 nM ).

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. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.

PROTAC ERα Degrader-2 is composed of a cIAP1 ligand binding group, a linker, and an estrogen receptor α (ERα) binding group, serving as an ERα degrader. It achieves maximal ERα degradation in human mammary tumor MCF7 cells at a concentration of 30 μM. Degradation inducers that utilize cIAP1 are referred to as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) (IC50 of 6.5 nM).

Degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS/FLI-expressing Ewing sarcoma cells. Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use. Negative control dTAGV-1-NEG (Cat. No. 6915) also available. FKBP12F36V can be expressed as a fusion with a target protein of interest using genome engineering techniques, via transgene expression or CRISPR-mediated locus-specific knock-in. Custom knock-in cell lines for the dTAG and aTAG platforms are available from our sister brand R&D Systems. Email TPD@bio-techne.com to enquire. Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.

PROTAC TG2 degrader-2 (compound 7) is a selective competitive degrader of Transglutaminase 2 (TG2), exhibiting a dissociation constant (Kd) greater than 100 μM. It inhibits cell migration and reduces TG2 levels in ovarian cancer cells, making it a valuable tool for ovarian cancer research [1].

PROTAC TTK Degrader-2 is a potent threonine tyrosine kinase (TTK) PROTAC degrader, achieving DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. It demonstrates effective target degradation and anticancer activity in a COLO-205 human colorectal cancer cell xenograft mouse model [1].

PROTAC EGFR degrader 7 (compound 13b) is a potent, selective, CRBN-recruiting EGFRL858R/T790M degrader with a DC50 of 13.2 nM. It effectively inhibits proliferation of NCI-H1975 cells with an IC50 of 46.82 nM, induces apoptosis, and causes a G2/M phase arrest in these cells. Demonstrating antitumor activity, this compound is applicable in non-small cell lung cancer (NSCLC) research.

PROTAC BRD9 Degrader-3 is a bifunctional degrader targeting BRD9, utilized in cancer research.

FMF-06-098-1 is a multitargeted depressant capable of promoting the degradation of a wide array of kinases, including AAK1, ABL2, AURKA, AURKB, BUB1B, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDK6, CDK7, CDK9, CHEK1, CSNK1D, EPHA1, PAK, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, SGK2, STK35, TNK2, UHMK1, ULK1, and WEE1 [1].

SNIPER(BRD)-1 is a chemical compound composed of a derivative of the IAP antagonist LCL-161 and the BET inhibitor (+)-JQ-1, linked together. It promotes the degradation of BRD4 through the ubiquitin-proteasome pathway and effectively degrades cIAP1, cIAP2, and XIAP with IC50 values of 6.8 nM, 17 nM, and 49nM, respectively[1].

PROTAC RIPK degrader-6 (example 1) is a PROTAC designed for the targeted degradation of RIP Kinase, featuring a RIP2 kinase inhibitor connected through a linker to a cereblon binder[1].

PROTAC EGFR degrader 7 (compound 13b) is a potent, selective CRBN-recruiting agent targeting EGFR L858R/T790M mutations with a DC50 of 13.2 nM. It effectively inhibits proliferation in NCI–H1975 cells with an IC50 of 46.82 nM and significantly triggers apoptosis and G2/M phase arrest in these cells. Demonstrating antitumor efficacy, PROTAC EGFR degrader 7 holds promise for non-small cell lung cancer (NSCLC) research [1].

PROTAC EED degrader-1 is a PROTAC targeting EED (pKD = 9.02), is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.17.

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

PROTAC Her3-binding moiety 1 is a Her3 Ligand for PROTAC.

Negative control for dTAGV-1.

BCL6 PROTAC 1 is a selective B-cell lymphoma 6 (BCL6) proteolysis targeting chimera (PROTAC) that inhibits the BCL6 cell reporter with an IC50 value of 8.8 µM and significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines, making it valuable for tumor-related research [1].

PROTAC EZH2 Degrader-1 (Compound 150d), a potent inhibitor, effectively suppresses EZH2 methyltransferase activity, demonstrating an IC50 of 2.7 nM. EZH2 is crucial in various tumorigenesis and development processes [1].

SNIPERTACC3-1 hydrochloride, an IAP ligand-based compound, selectively degrades the TACC3 protein through the ubiquitin-proteasome pathway, thereby inducing cancer cell apoptosis [1].

PROTAC TTK degrader-1, a potent threonine tyrosine kinase (TTK) PROTAC degrader, demonstrates DC50 values of 1.7 nM in COLO-205 cells and 5.8 nM in HCT-116 cells, indicating effective target degradation. Furthermore, it shows anticancer efficacy in a xenograft mouse model with COLO-205 human colorectal cancer cells [1].

PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based degrader targeting BRD4, exhibiting a pDC50 of 9.2 in MOLT4 cells over 24 hours [1].

D-MoDE-A (1) is a bifunctional small molecule that facilitates extracellular protein degradation via the asialoglycoprotein receptor (ASGPR).

PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader with IC50 of 13.5 nM.

PROTAC EGFR degrader 2 is a potent compound with exceptional antiproliferative activity, evidenced by its IC50 of 4.0 nM, and exhibits strong EGFR degradation activity with a DC50 of 36.51 nM. It is suitable for synthesizing nitroreductase (NTR)-responsive PROTACs [1].

PROTAC AR-V7 degrader-1 (Compound 6) is an orally bioavailable, potent, and selective degrader targeting the androgen receptor (AR) variant V7, achieving degradation with a DC50 of 0.32 µM by directing the VHL E3 ligase to the AR DNA-binding domain (DBD). It demonstrates efficacy in the 22Rv1 cell line expressing AR-V7, with an EC50 of 0.88 µM [1].

PROTAC PTPN2 Degrader-1 (compound example 77) is a potent entity capable of degrading PTPN2, showing promise for research applications in cancer or metabolic diseases [1].

PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC 50 of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research [1] .

1-Bromo-6-chlorohexane (Hexane, 1-bromo-6-chloro-) is used as PROTAC linker.

dTAGV-1 TFA is a highly effective and specific compound that targets mutant FKBP12 F36V fusion proteins for degradation. It possesses potent activity in inducing the degradation of the FKBP12 F36V -Nluc protein in living organisms.

Homo-PROTAC cereblon degrader 1 is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.

SMARCA-BD ligand 1 for Protac dihydrochloride binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.

PROTAC PARP1 degrader is a degrader of PARP1 based on the PROTAC technology. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line (IC50 of 6.12 μM).

UAA crosslinker 1 hydrochloride is an amber codon used to incorporate non-canonical amino acids (ncAAs) into proteins in vivo. This is achieved by leveraging the promiscuous activity of specific wildtype and engineered aminoacyl-tRNA synthetases[1].