protac mdm-2 degrader-2

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].

1,2-Bis(2-iodoethoxy)ethane is a PEG-based PROTAC linker used in the synthesis of MT802 and SJF620, which are potent PROTAC BTK degraders with DC50s of 1 nM and 7.9 nM, respectively [1].

5-Ethynyl-2'-deoxyuridine (EdU) is a nucleoside analog of thymidine used to monitor de novo DNA synthesis through click chemistry and serves as an alkyl chain-based PROTAC linker for synthesizing PROTACs.

2-Phthalimidehydroxy-acetic acid is an alkyl chain-based PROTAC linker utilized in PROTAC synthesis.

dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, binding to MCL1 with a KD of 30 nM and activating the apoptosis mechanism by degrading MCL1.

PROTAC ERRα ligand 2 is an inverse agonist for the estrogen-related receptor α (ERRα) with an IC50 of 5.67 nM.

TSPO ligand-2 (Carbonic acid) is a ligand of AUTAC1 which contains a p-fluorobenzylguanine and a Fumagillol moiety.

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

Hydroxy-PEG4-(CH2)2-Boc is an uncleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs) and can also be employed in the synthesis of PROTAC.

PROTAC MDM2 Degrader-3 utilizes PROTAC technology to degrade MDM2 by combining a potent MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].

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

PROTAC BET-binding moiety 2 is an inhibitor of the BET bromodomain.

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].

SNIPER(TACC3)-2 targets TACC3 protein degradation via the ubiquitin-proteasome pathway. It induces cancer cell death.

Thalidomide-O-amido-PEG1-(C1-PEG)2-C2-NH2 is a synthesized E3 ligase ligand-linker, incorporating a cereblon ligand based on Thalidomide and a 3-unit PEG linker, specifically designed for PROTAC technology applications.

6-O-2-Propyn-1-yl-D-galactose functions as an irreversible glycolinker, facilitating the attachment of cytotoxic drugs for applications in antibody-drug conjugation (ADC).

Bis (2-bromoethyl) ether, an alkyl chain-derived PROTAC linker, facilitates the synthesis of PROTACs.

Bis-Tos-(2-hydroxyethyl disulfide) is a cleavable linker used in the synthesis of antibody-drug conjugates (ADCs) [1].

DBCO-(PEG2-Val-Cit-PAB)2 is a dual-cleavable linker used in antibody-drug conjugates (ADCs).

GID4 Ligand 2 (compound 67) is a selective binder for GID4 with an IC50 of 18.9 μM and a Kd of 17 μM, and can be used for the synthesis of PROTACs [1].

PROTAC RAR Degrader-1, an RAR degrader, consists of a cIAP1 ligand binding group, a linker, and an RAR ligand binding group. It achieves maximal RAR degradation at a concentration of 30 μM in HT1080 cells. Degradation inducers that utilize cIAP1 are known as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

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

PROTAC BTK Degrader-3 is a potent degrader of Bruton's tyrosine kinase (BTK), with a DC50 (median degradation concentration) of 10.9 nM in Mino cells, and shows promise for research into B-cell malignancies, such as chronic lymphoid malignancies [1].

PROTAC MLKL Degrader-1 (Compound 36) is a selective PROTAC degrader targeting MLKL, with a degradation maximum (D max) exceeding 90%. The compound incorporates modified cereblon (CRBN) ligands and a lenalidomide-linker within its structure, effectively inhibiting cell death in a TSZ-induced model of necroptosis.

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

(2-Pyridyldithio)-PEG4-alcohol, a PEG-based PROTAC linker, is used for the synthesis of PROTACs[1].

PROTAC BRD9 Degrader-1 is a leading PROTAC BRD9 chemical degrader with an IC50 of 13.5 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].

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 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].

RIPK2-IN-2 (example 25) is a RIP2 kinase PROTAC inhibitor that effectively blocks RIP2-dependent pro-inflammatory signaling and regulates RIP2 kinase activity in autoinflammatory diseases [1].

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].

4-Methyl-4-(pyridin-2-yldisulfanyl)pentanoic acid is a cleavable linker compound used in the synthesis of antibody-drug conjugates (ADCs) [1].

PEG6-(CH2CO2H)2 is a symmetric PEG PROTAC linker.

YX-2-107 is a selective and potent CDK6-degrading PROTAC with an IC50 value of 4.4 nM.YX-2-107 inhibits RB phosphorylation and FOXM1 expression in vitro, and inhibits the development of Ph+ ALL in rats.YX-2-107 can be used for the prophylaxis and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). YX-2-107 can be used for the prevention and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL).

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

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

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).

Compound 72-1, also known as BCL-xL BCL-2 ligand 1, serves as a ligand for BCL-xL and BCL-2 proteins. It can be tethered to an E3 ligase via a linker, facilitating the formation of PROTACs [1] [2].

VEGFR-2-IN-39 (PROTAC-5), a PROTAC that targets VEGFR-2 with an IC 50 of 208.6 nM, demonstrates low toxicity. It effectively inhibits the proliferation of EA.hy926, a type of HUVEC, in a concentration-dependent manner, achieving an IC 50 value of 38.65 µM [1].

cIAP1 Ligand-Linker Conjugates 2 is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a PROTAC linker. This compound is particularly useful in the design of SNIPERs [1].

PROTAC BRD4 Ligand-2 Hydrochloride serves as a ligand targeting the BRD4 protein, specifically designed for use with PROTAC CFT-2718.

PROTAC α-synuclein degrader 3 (compound 5) is a potent and selective agent for degrading α-synuclein, used in Parkinson's disease research [1].

PROTAC BRD4 Degrader-16 is a potent degrader of BRD4, with IC50 values of 34.58 nM for BRD4 (BD1) and 40.23 nM for BRD4 (BD2). It significantly reduces Cyclin B1 expression, impedes G2 M phase progression, and induces apoptosis in MV-4-11 cells [1].

PROTAC TG2 Degrader-1 (Compound 11) is a VHL-based PROTAC that targets tissue transglutaminase (TG2) and exhibits a binding affinity with a K D of 68.9 μM. This compound effectively decreases TG2 levels in ovarian cancer cells through a proteasome-dependent pathway [1].

PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1 2 phosphorylation. With a pIC50 value of 7.0, it exhibits antiproliferative activity against A375 cells [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.