protac pd-1/pd-l-1 degrader-1

PROTAC PD-1 PD-L1 degrader-1, a Cereblon E3 ligand-based compound, is a PD-1 PD-L1 PROTAC that effectively inhibits the PD-1 PD-L1 interaction with an IC50 of 39.2 nM. It restores the suppressed immune response in a co-culture model of Hep3B OS-8 hPD-L1 cells and CD3 T cells and moderately decreases PD-L1 protein levels through a lysosome-dependent mechanism.

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

SMARCA-BD ligand 1 for Protac is a compound that binds to SMARCA2, the BAF ATPase subunit, utilizing Protac technology to degrade SMARCA2.

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

N-Boc-4-pentyne-1-amine is an alkyl chain-based PROTAC linker compound used in the synthesis of PROTAC MG-277 [1].

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

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.

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

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.

CRBN modulator-1 (WUN29654) is a Thalidomide analog and CRBN modulator,has an IC50 of 3.5 μM and a Ki of 0.98 μM.

PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.

BRD7-IN-1, a modified derivative of BI7273 (BRD7 9 inhibitor), forms PROTAC VZ185 via linkage to a VHL ligand, demonstrating potent activity against BRD7 9 with DC50 values of 4.5 and 1.8 nM, respectively [1].

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 subunit SMARCA2 and is used for degrading SMARCA2 based on PROTAC.

Homo-PROTAC pVHL30 degrader 1 is a potent PROTAC-based degrader of pVHL30.

PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50 values of 0.04 μM for ERRα and 2.8 μM for ERRγ.

PROTAC CBP P300 Degrader-1 is an effective compound that potently degrades CBP P300, significantly reducing cell viability in various cancer cell lines.

PROTAC IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].

PROTAC BRD4 Degrader-9 (compound 8a) is a novel chemical compound comprising ligands for von Hippel-Lindau and BRD4, connected by a PROTAC moiety. This compound efficiently degrades the BRD4 protein in PC3 prostate cancer cells. When conjugated with STEAP1 and CLL1 antibodies, PROTAC BRD4 Degrader-9 exhibits potent activity, with respective DC50 values of 0.86 nM and 7.6 nM.

CDK9 Antagonist-1 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

1-Boc-azetidine-3-carboxylic acid is a valuable organic compound for life sciences research (catalog number T67359, CAS number 142253-55-2).

PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC coupler that targets SGK3 and binds ligand to VH032 VHL, inducing degradation of endogenous SGK3. It inhibits GDC0941-induced proliferation of cancer cells. [CAS 번호5017-88-83-4]

PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein, reducing its levels by >80% at a concentration of 30 nM. Notably, this compound shows no activity against the ERRβ and ERRγ proteins.

1-Cbz-3-Hydroxyazetidine (catalog number: T66502, CAS number: 128117-22-6) is a valuable organic compound for life sciences research.

PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1.

PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).

PROTAC BRD9-binding moiety 1 hydrochloride inhibits BRD9 activity by binding to BRD9, utilizing the PROTAC (Proteolysis Targeting Chimera) mechanism.

MV-1-NH-Me, an MV-1-derived IAP ligand, connects to an ABL inhibitor through a linker, resulting in the formation of SNIPER[1].

(rel)-PROTAC ERRα Degrader-1, a relative configuration of PROTAC ERRα Degrader-1, is an estrogen-related receptor alpha (ERRα) degrader comprising an MDM2 ligand binding moiety, a linker, and an ERRα binding moiety [1].

Halo PROTAC 1 is a PROTAC, which is a ligand having activity to bind to an intracellular proteins fused with HaloTag and a structure having activity to induce autophagy of an intracellular molecule are linked via a PEG linker[1].

S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate, an ADC linker, is a glutathione-cleavable compound used for attaching monoclonal antibodies (mAb) in antibody-drug conjugates (ADCs), specifically referring to the Alkyl-Chain composition of the linker portion of these molecules [1].

cIAP1 Ligand-Linker Conjugates 1 is composed of an IAP ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound, cIAP1 Ligand-Linker Conjugates 1, is particularly useful in the development of SNIPERs[1].

1-(t-Boc-Aminooxy)-3-aminooxy-propane is an alkyl ether-based PROTAC linker used in the synthesis of PROTACs [1].

PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27) and an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.11.

PROTAC EGFR degrader 4 is a potent molecule designed to target and degrade mutant EGFR, effectively inducing degradation of EGFR del19 and EGFR L858R T790M with DC50 values of 0.51 nM and 126 nM, respectively. It significantly inhibits the growth of HCC827 and H1975 cell lines, demonstrating IC50 values of 0.83 nM and 203.1 nM, respectively. The induced degradation of EGFR by this compound is associated with autophagy [1].

PROTAC EGFR degrader 6 is a potent PROTAC EGFR degrader that effectively reduces EGFR Del19 levels in HCC827 cells, exhibiting a DC50 of 45.2 nM. It notably promotes apoptosis and induces G1 phase arrest in HCC827 cells [1].

PROTAC SOS1 degrader-1, a potent compound, demonstrates an effective degradation of PROTAC SOS1 with a DC50 value of 98.4 nM. It exhibits antiproliferative activity against cancer cells harboring diverse KRAS mutations and has shown an antitumor effect with low toxicity [1].

PROTAC PTK6 ligand-1 serves as an intermediate in the synthesis of BTK kinase inhibitors [1] and is utilized in the preparation of ARD-61 [2].

1-(Isopropylthio)-2,3,4,6-tetra-O-Ac-beta-D-glucosylpyranose is an alkyl chain-derived PROTAC linker used in the synthesis of PROTACs[1].

PROTAC CDK9 degrader-7 is a proteolysis-targeting chimera (PROTAC) engineered to selectively target and mediate the degradation of Cyclin-Dependent Kinase 9 (CDK9) via the proteasome pathway [1].

PROTAC CDK9 degrader-5 is a selective PROTAC that mediates degradation of CDK9 via the proteasome pathway, efficiently degrading CDK9 42 and CDK9 55 isoforms with DC50 values of 0.10 μM and 0.14 μM, respectively [1].

Compound A6, a potent and selective PROTAC HDAC6 degrader, exhibits a DC50 of 3.5 nM. It demonstrates notable antiproliferative activity by inducing apoptosis in myeloid leukemia cell lines [1].

GID4 Ligand 1 is a cell-permeable, highly selective GID4 binder with an IC50 value of 5.4 μM and a Kd value of 5.6 μM. GID4 Ligand 1 is capable of binding GID4 in cells with an EC50 value of 558 nM. GID4 Ligand 1 is capable of being used in the synthesis of PROTACs.

PROTAC MDM2 Degrader-4, designed using PROTAC technology, combines a potent MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase to degrade MDM2[1].

PROTAC FKBP Degrader-3 is a potent FKBP degrader, consisting of a FKBP ligand binding group, a linker, and a VHL binding group [1].

PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf,PROTAC B-Raf degrader 1 With anti-cancer activity.

PROTAC BTK Degrader-6 (Compound 15), with a DC50 of 3.18 nM, exhibits anti-inflammatory properties by inhibiting NF-κB activation and suppressing the expression of pro-inflammatory cytokines such as IL-1β and IL-6 [1].