protac crabp-ii degrader-3

PROTAC CRABP-II Degrader-3 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on [cIAp1].

Gefitinib-based PROTAC 3, which connects 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 mutation) cells, respectively[1].

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

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

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

PROTAC tubulin-Degrader-1 (Compound W13) functions as an inhibitor of PROTAC tubulin and exhibits anti-tumor activity against human lung cancer.

PROTAC ERα Degrader-4, a highly potent and selective agent (K i: 5.08 μM), contains OBHSAs, a linker, and E3 ligase ligands. This compound demonstrates superb inhibitory effects and ERα degradation activity in both Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells, as well as in ERα-mutated BC cells. Additionally, PROTAC ERα Degrader-4 can induce apoptosis, making it valuable for cancer research.

PROTAC KRAS G12C degrader-2 (compound 432) acts as a bifunctional modulator, enhancing the hydrolysis of K-Ras protein. One end of this compound features a cereblon inhibitor of apoptosis proteins (IAP), while the other end contains a moiety that binds to KRAS [1].

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].

PROTAC EGFR degrader 8 (T-184) is a PROTAC that selectively degrades the epidermal growth factor receptor (EGFR) with a DC50 of 15.56 nM in HCC827 cells, and inhibits the growth of cell lines H1975, PC-9, and HCC827 with IC50 values of 7.72 nM, 121.9 nM, and 14.21 nM, respectively. This compound is used primarily for cancer research, particularly in the context of non-small cell lung cancer (NSCLC) [1].

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

PROTAC NSD3 degrader-1 (compound 56) is a targeted degradation agent for the Nuclear receptor binding SET domain protein NSD3. It effectively induces NSD3 degradation 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, arrests the cell cycle, and 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 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].

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].

HDAC6 degrader-3, a selective and potent degrader of HDAC6 through ternary complex formation and the ubiquitin-proteasome pathway, exhibits a DC50 value of 19.4 nM. With IC50 values of 4.54 nM for HDAC6 and 0.647 μM for HDAC1, it effectively induces robust hyperacetylation of α-tubulin [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].

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 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.

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.

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).

(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].

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 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 BET Degrader-1 is a potent BET degrader utilizing the PROTAC mechanism.

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

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 BRD4 Degrader-20 (compound 195) is a bifunctional degrader of BRD4 [1].

PROTAC ERα Degrader-8 (compound ii-56), a highly potent degrader of Erα, achieves a DC50 of just 0.000006 μM in MCF7 cells [1].

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 CDK9 Degrader-8 (Compound 21) is a potent degrader of CDK9 with an IC50 of 0.01 μM, utilized in cancer research [1].

PROTAC SOS1 Degrader-4 (compound 10) is a potent degrader of SOS1 and exhibits antiproliferative activity [1].

PROTAC CDK4 6 degrader 1 (Compound 7f) is a dual degrader of CDK4 and CDK6, with DC50 values of 10.5 nM and 2.5 nM, respectively. This compound effectively inhibits proliferation in Jurkat cells (IC50 of 0.18 μM), induces cell cycle arrest during the G1 phase, and triggers cell apoptosis (apoptosis). It features a pink ligand for target protein YY173, a black linker, and a blue ligand for E3 ligase.

PROTAC ATR degrader-2 (Compound 8i) serves as a PROTAC degrader targeting ATR, effectively degrading it in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, with DC50 values of 22.9 and 34.5 nM, respectively. This compound induces apoptosis and inhibits the proliferation of AML cells. Additionally, PROTAC ATR degrader-2 demonstrates favorable pharmacokinetic properties and potent antitumor activity in a mouse model of AML. (Pink: ATR ligand; Blue: E3 ligase ligand Lenalidomide; Black: linker) [1]

PROTAC CDK9 Degrader-1 is a selective degrader of cyclin-dependent kinase 9 (CDK9).

PROTAC BRD4 Degrader-21 (Comp 74), a potent BRD4 degrader, has shown significant inhibition of tumor growth in mouse xenograft models, indicating its potential for anticancer research [1].

PROTAC TG2 degrader-2 (compound 7) is a selective competitive degrader of Transglutaminase 2 (TG2) with 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].