protac sgk3 degrader1

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]

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

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

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.

SMARCA-BD ligand 1 for Protac dihydrochloride binds to the BAF ATPase subunit SMARCA2 and is used for degrading SMARCA2 based on PROTAC.

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

PROTAC IRAK3 Degrade-1 (Compound 23) is a selective and potent IRAK3 degrader, demonstrating an IC50 value of 5 nM [1].

Methyl 1-Cbz-azetidine-3-carboxylate acts as a stable ADC linker for synthesizing antibody-drug conjugates (ADCs) and as an alkyl chain-based PROTAC linker in developing PROTACs[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 α-synuclein degrader 3 (compound 5) is a potent and selective agent for degrading α-synuclein, used in Parkinson's disease research [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 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].

1-Boc-azetidine-3-yl-methanol [catalog number T66497, CAS number 142253-56-3] is a valuable organic compound for life sciences research.

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 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 Hemagglutinin Degrader-1 (Compound V3) is a potent degrader of influenza hemagglutinin (HA) with a median degradation concentration of 1.44 μM and broad-spectrum anti-influenza virus activity [1].

PROTAC FLT3/CDK9 degrader-1, a potent dual degrader of FLT3 and CDK9, effectively induces apoptosis and targets protein degradation of FLT3 and CDK9. This compound holds research potential for FLT3-ITD mutated AML [1].

PROTAC GPX4 Degrader-1 (DC-2) is a PROTAC-based compound that efficiently degrades GPX4, demonstrating a degradation concentration (DC 50) of 0.03 μM in HT1080 cells [1].

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 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).

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].

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].

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 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 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 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 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].

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 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].

SMARCA-BD Ligand 1 Hydrochloride, used in PROTAC technology, targets and binds to the BAF ATPase subunits SMARCA2, facilitating its degradation.

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

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].