protac brd9 binding moiety 1 hydrochloride

PROTAC BRD9-binding moiety 1 hydrochloride binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.

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.

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.

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

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

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 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.

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

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].

PROTAC NSD3 degrader-1 (compound 56) is a targeted degradation agent for the Nuclear receptor binding SET domain protein NSD3. It effectively induces the degradation of NSD3 in NCI-H1703 and A549 lung cancer cell lines, with DC50 values of 1.43 and 0.94 μM, respectively. Additionally, it hinders H3K36 methylation, triggers apoptosis, and arrests the cell cycle. Furthermore, PROTAC NSD3 degrader-1 diminishes the expression of NSD3-related genes, including CDC25A, ALDH1A1, and IGFBP.

PROTAC GDI2 Degrader-1 (Compound 21) is a potent degrader of PROTAC GDI2, demonstrating outstanding antitumor activity in vivo within pancreatic xenograft models that overexpress GDI2 [1].

PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.

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

PROTAC CBP/P300 Degrader-1 is an effective compound that degrades CBP/P300 in a potent manner. It significantly reduces cell viability in various cancer cell lines.

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

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].

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.

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].

PROTAC K-Ras Degrader-1 is potent degrader of K-Ras based PROTAC.

PROTAC BTK Degrader-1, a powerful, selective, and orally bioavailable degrader of PROTAC BTK, demonstrates effective reduction in BTK protein levels and tumor suppression. It exhibits IC50 values of 34.51 nM for BTK WT and 64.56 nM for BTK-481S, highlighting its potency and efficacy in targeting and diminishing BTK protein abundance [1].

PROTAC MLKL Degrader-1 (Compound 36) is a selective PROTAC degrader targeting MLKL, achieving a degradation maximum (D max) over 90%. The compound encompasses modified cereblon (CRBN) ligands and a lenalidomide-linker as part of its structure. It effectively inhibits cell death in a TSZ-induced model of necroptosis.

PROTAC KRAS G12C degrader-1, a cereblon-based degrader, promotes CRBN/KRAS G12C dimerization and facilitates the degradation of GFP-KRAS G12C in reporter cells [1].

PROTAC BRD9 Degrader-7 is a selective and orally active BRD9 degrader with a DC50 of 1.02 nM and demonstrates superior pharmacokinetics, evidenced by a Cmax of 3436.95 ng/mL [1].

PROTAC BRD9 Degrader-5 is a proteolysis targeting chimera (PROTAC) designed for the specific degradation of Bromodomain-containing protein 9 (BRD9).

PROTAC IRAK3 degrade-1 is a potent and selective degrader of IRAK3 ( IC 50 = 5 nM).

CDK ligand for PROTAC hydrochloride is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.

PROTAC CDK9 Degrader-1 is a selective CDK9 degrader.

PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule belonging to the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal domain (AR-NTD) of the Androgen Receptor variant AR-V7. By antagonizing AR-NTD, this compound effectively degrades AR-V7 protein and triggers apoptosis in prostate cancer (PC) cells, with degradation efficiencies in VCaP cells recorded at 62.2% (1 μM) and 71.1% (5 μM), as noted in reference [1].

PROTAC pan-IAP degrader-1 (Compound 9) is a pan- IAP degrader PROTAC . PROTAC pan-IAP degrader-1 degrades XIAP , cIAP1 and cIAP2 with DC 50 s of 0.7, 2.4, and 6.2 nM in MM.1S cells, respectively [1] .

9-Decyn-1-ol is an alkyl/ether-based PROTAC linker suitable for synthesizing PROTACs. It serves as a conjugation agent to combine GDC-0068 and Lenalidomide, resulting in the formation of INY-03-041. INY-03-041 is a potent and highly selective pan-Akt degrader that operates through the PROTAC mechanism. It effectively inhibits Akt1, Akt2, and Akt3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively[1].

PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).

PROTAC BRD9 Degrader-6, with an IC50 value of 0.13 nM, is a potent degrader of BRD9 suitable for research on BAF complex-related disorders [1].

Compound X10g (PROTAC Hsp90α degrader 1) is a selective agent targeting Hsp90α for degradation and is utilized in breast cancer research. It demonstrates inhibitory effects on the proliferation of breast cancer cell lines, MDA-MB-231, MDA-MB-468, MCF-7, and MX-1, with respective IC50 values of 51.48 μM, 16.46 μM, 8.93 μM, and 11.95 μM [1].

PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4.

PROTAC MDM2 Degrader-1 is a chemical compound that utilizes PROTAC technology to degrade MDM2. This compound is comprised of a highly effective MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].

PROTAC CRABP-II Degrader-1 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on cIAp1.

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.

PROTAC PARP/EGFR ligand 1 is a potent compound utilized in the creation of dual PARP-EGFR degraders through Proteolytic Targeting Chimera (PROTAC) technology [1].

PROTAC Axl Degrader 1 is a potent, selective degrader of PROTAC Axl, exhibiting an IC50 of 0.92 µM. It demonstrates in vitro anti-proliferative and anti-migratory activities and induces mehuosis [1].