erα degrader2

ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, exhibiting an EC50 value of 0.3 nM for ERα degradation. It can be used for the prevention and treatment of HER-positive breast cancer.

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 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].

ER degrader 6 (compound 35s) is a potent selective estrogen receptor modulator (SERM) with the capacity to degrade Estrogen Receptor (ER)α. It disrupts the microtubule network, inhibits tubulin polymerization, and effectively suppresses tumor growth with minimal toxicity [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.

ER degrader 1 is a potent degrader of the estrogen receptor (ER) with potential applications in cancer treatment, as it targets the estrogen signaling system, which is crucial for cell growth, differentiation, and apoptosis.

IKZF1-degrader-2 (Compound 3), an IKZF1 degrader, exhibits anticancer activity and low toxicity [1].

PROTAC ER Degrader-4 is a PROTAC degrader of the estrogen receptor (ER) with an IC50 of 0.8 nM.

STAT3 Degrader-2 is a PROTAC-based compound that effectively reduces the total STAT3 protein levels, and is utilized in the research of cancer and various diseases [1].

ER degrader 7 (Compound 35t) is a selective degrader of both ERα and ERβ and functions as a tubulin polymerization inhibitor. It inhibits cell viability with IC50 values of 0.06 μM for MCF-7, 2.56 μM for T47D, 15.84 μM for MCF-10A, 1.59 μM for LCC2, 1.67 μM for T47D D538G, and 1.37 μM for T47D Y537S cells. Additionally, ER degrader 7 demonstrates efficacy in suppressing breast cancer tumor growth [1].

PROTAC PTPN2 degrader-2 (example 187B) is a potent PTPN2-degrading agent with potential applications in cancer and metabolic disease research [1].

Androgen Receptor Degrader-2 (Compound 9) is a potent degrader of androgen receptors, with potential application in cancer research [1].

PROTAC SMARCA2 degrader-2, a selective and powerful degrader of SMARCA2/4, exhibits an IC50 of <0.1 μΜ in the HeLa HiBiT assay.this compound holds promise for research into cancers related to or deficient in SMARCA4 [1].

PROTAC BRAF-V600E degrader-2 is a useful organic compound for research related to life sciences. The catalog number is T8744 and the CAS number is 2417296-82-1.

PROTAC SOS1 degrader-2, a potent degrader of PROTAC SOS1, effectively reduces the expression of pERK and RAS-GTP in a dose-dependent manner. It significantly inhibits tumor growth in vivo [1].

PROTAC ER Degrader-10 is a potent PROTAC ER degrader, suitable for cancer research.

ER degrader 3, a potent estrogen receptor (ER) degrader, significantly impacts the estrogen signaling pathway, which is crucial for regulating cell growth, differentiation, and apoptosis. This compound holds potential for cancer research[1].

Nampt degrader-2, a fluorescent PROTAC, exhibits efficient degradation of NAMPT at an IC50 of 41.9 nM. It operates by binding to both NAMPT and VHL, initiating the formation of a ternary complex that triggers NAMPT degradation through the ubiquitin-proteasome system (UPS). This activity significantly lowers NAD+ levels and displays potent antitumor effects [1].

GSPT1 degrader-2 is a potent degrader of GSPT1 [1].

PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group. This compound is designed to specifically degrade estrogen-related receptor alpha (ERRα), acting as an ERRα degrader[1].

ER Degrader 2, a potent estrogen receptor (ER) degrader, plays a significant role in the estrogen signaling system, which is crucial for regulating cell growth, differentiation, and apoptosis. It holds promise for research in cancer diseases[1].

PROTAC STAT3 degrader-2 is a selective and effective PROTAC degrader of the STAT3 protein, exhibiting a DC50 of 3.54 μM in Molm-16 cells. It holds potential for cancer research [1].

PROTAC Bcl-xL degrader-2, based on von Hippel-Lindau ligand, is a potent degrader of Bcl-xL (a Bcl-2 family member), demonstrating an IC 50 of 0.6 nM.

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

ER Degrader 5 is a potent compound that degrades the estrogen receptor (ER), exhibits anti-proliferation activity, and has potential applications in breast cancer research [1].

PROTAC VEGFR-2 Degrader-1 (PROTAC-1), a specific degrader of PROTAC VEGFR-2, demonstrates minimal inhibition of VEGFR-2 (IC50 > 1 μM) and exhibits low anti-proliferative effects on EA.hy926 cells (IC50 > 100 μM) [1].

PROTAC VEGFR-2 degrader-2 (PROTAC-4), a specific degrader of VEGFR-2, demonstrates minimal inhibition of VEGFR-2 (IC50 > 1 μM) and low anti-proliferative activity towards EA.hy926 cells (IC50 > 100 μM) [1].

PROTAC MDM2 Degrader-2, designed using PROTAC technology, functions as a MDM2 degrader. It consists of a highly potent MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase, facilitating the degradation of MDM2[1].

PROTAC BRD3 BRD4-L degrader-2, a PROTAC molecule, selectively degrades cellular BRD3 and BRD4-L with K i values of 16.91 and 2.8 nM, respectively, and exhibits robust antitumor activity in mouse xenograft models, serving as a research tool for cancer [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].

ER degrader 4, a selective and orally active compound, effectively degrades estrogen receptors and exhibits anti-tumor activity [1].

PROTAC BTK Degrader-2, a potent degrader of BTK through the PROTAC mechanism, effectively diminishes BTK protein levels [1].

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 CRABP-II Degrader-2 is a potent cIAp1-based degrader of cellular retinoic acid binding protein (CRABP-II).

PROTAC CARM1 degrader-2 (compound 3e), with a DC50 value of 8.8 nM, is a VHL- and proteasome-dependent degrader of co-activator associated arginine methyltransferase (CARM1). It promotes the degradation of CARM1 and prevents the methylation of its substrates, including poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, consequently inhibiting breast cancer cell migration [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].

PROTAC CDK9/CycT1 Degrader-2 inhibits CDK9 with an IC50 of 45 nM [1].

PROTAC PTPN2 degrader-2 (example 187B) TFA is a potent Protein Tyrosine Phosphatase Non-receptor Type 2 (PTPN2) degrader with potential applications in cancer and metabolic disease research [1].

PROTAC BRD9 Degrader-2 is a bifunctional compound engineered for the targeted degradation of BRD9 (Bromodomain containing 9) in cancer research applications.

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

PROTAC ER Degrader-3, an intermediate for the synthesis of PAC, specifically compound LP2. PAC serves as the linker for ADCs and PROTACs that are conjugated to an antibody. Notably, when PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) compared to PROTAC alone [1].

PROTAC ER Degrader-2 serves as a synthesis intermediate for the production of PAC, a compound that incorporates the ADCs linker and PROTACs, which are subsequently conjugated to an antibody. PAC, exhibits a greater capability to degrade estrogen receptor-alpha (ERα) compared to PROTAC (without the presence of an antibody)[1].

PROTAC CDK9 degrader-2 (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].

PROTAC Axl Degrader 2, a potent and selective PROTAC Axl degrader, demonstrates an IC50 of 1.61 µM. It exhibits anti-proliferative and anti-migratory activities in vitro and induces mehuosis [1].

PROTAC IRAK4 Degrader-2 (Compound 9) is a PROTAC-based degrader that potently reduces IRAK4 levels, achieving a DC50 of 151 nM in peripheral blood mononuclear cells (PBMCs). It also notably decreases IRAK4 protein levels with a DC50 of 36 nM in the same cell type and inhibits several cytokines in PBMCs [1].