pomalidomide-c2-amido-(c1-o-c5-o-c1)2-cooh

Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a chemically synthesized compound, designed as an E3 ligase ligand-linker conjugate, integrating the cereblon ligand derived from Pomalidomide and a linker employed in PROTAC technology. This compound serves to facilitate targeted protein degradation through the modulation of E3 ligase activity, enabling the selective elimination of specific proteins of interest.

(+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1/2) (IC50=77/33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

Boc-NH-O-C1-NHS ester is an alkyl/ether-based PROTAC linker that can be used in PROTAC synthesis.

2-Phthalimidehydroxy-acetic acid is an alkyl chain-based PROTAC linker that can be used in PROTAC synthesis.

2,3,4,6-Tetra-o-acetyl-alpha-galactosylpyranosyl bromide (2-3-4-6-tetra-o-acetyl-alpha-galactosylpyranosyl-bromide) is an alkyl chain-based PROTAC linker that can be used in PROTAC synthesis.

Pomalidomide-C4-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

Thalidomide-O-amido-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate, integrating a Thalidomide-based cereblon ligand with a linker, suitable for PROTAC synthesis.

Pomalidomide-CH2CONH-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.

Thalidomide-O-CH2CONH-CH2COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based CRBN ligand and linker used in PROTAC technology.

2-(2,6-dioxopiperidin-3-yl)-4-((9-hydroxynonyl)oxy)isoindoline-1,3-dione is a PROTAC linker that can be used in the synthesis of PROTACs.

Pomalidomide-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.

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

Pomalidomide-C5-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based CRBN ligand and linker used in PROTAC technology.

2-(2,6-dioxopiperidin-3-yl)-4-((7-hydrox is protac.

Cl-C6-PEG4-O-CH2COOH (PROTAC Linker 4) is an effective pegylated PROTAC linker, which is often used in PROTAC synthesis of chloroanes (HaloPROTACs).

PROTAC BRD4 ligand-1 is a ligand for PROTAC GNE-987 targeting the BRD4 protein and is an inhibitor of BET.

Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, which binds to MCL1 with a KD of 30 nM. dmcl-2 activates the apoptosis mechanism by degrading MCL1.This compound is unstable in powder form and other related salt forms are recommended.

dCBP-1 is a chemical degrader of p300 CBP. dCBP-1 hijacks the E3 ubiquitin ligase CRBN for selective degradation of p300 CBP. Degradation of p300 CBP by dCBP-1 leads to effective multiple myeloma cell killing.

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

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].

Thalidomide-O-C8-COOH, also known as Cereblon ligand 3, is a Thalidomide-derived compound that serves as a Cereblon (CRBN) ligand for the targeted recruitment of CRBN protein. It can be coupled via a linker to another ligand to create proteolysis-targeting chimeras (PROTACs)[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.

Cereblon inhibitor 1, an isoindoline derivative, serves as a modulator of the cereblon E3 ubiquitin ligase and shows promise for applications in cancer research.

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

1-Isothiocyanato-PEG3-azide is a PEG-based PROTAC linker utilized for PROTAC synthesis[1].

U7D-1, a groundbreaking and selective ubiquitin-specific protease 7 (USP7) PROTAC degrader, exhibits a DC50 value of 33 nM in RS4;11 cells, demonstrating its potent anticancer properties. Furthermore, U7D-1 effectively induces apoptosis in Jeko-1 cells [1].

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

PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins (IC50 of 9.6 nM ).

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.

AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG molecules[1].

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

Degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS/FLI-expressing Ewing sarcoma cells. Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use. Negative control dTAGV-1-NEG (Cat. No. 6915) also available. FKBP12F36V can be expressed as a fusion with a target protein of interest using genome engineering techniques, via transgene expression or CRISPR-mediated locus-specific knock-in. Custom knock-in cell lines for the dTAG and aTAG platforms are available from our sister brand R&D Systems. Email TPD@bio-techne.com to enquire. Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.

Thalidomide-O-amido-PEG4-azide is a polyethylene glycol (PEG) derivative serving as a linker for Proteolysis Targeting Chimeras (PROTACs) synthesis [1].

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

SHP2 protein degrader-2 (SHP2-D26), a PROTAC degrader targeting the SHP2 protein, effectively diminishes its expression levels across various cancer cell types [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].

FMF-06-098-1 is a multitargeted depressant capable of promoting the degradation of a wide array of kinases, including AAK1, ABL2, AURKA, AURKB, BUB1B, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDK6, CDK7, CDK9, CHEK1, CSNK1D, EPHA1, PAK, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, SGK2, STK35, TNK2, UHMK1, ULK1, and WEE1 [1].

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].

m-PEG6-2-methylacrylate is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

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.

DBCO-(PEG2-VC-PAB-MMAE)2 consists of Monomethyl auristatin E (MMAE), a toxin payload in antibody-drug conjugate [1], conjugated to the cleavable linker DBCO-(PEG2-VC-PAB)2. MMAE, a potent tubulin inhibitor, serves as the cytotoxic component in this formulation.

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

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

Propargyl-PEG4-O-C1-Boc is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

m-C-tri(CH2-PEG1-NHS ester) is a non-cleavable one-unit polyethylene glycol (PEG) linker employed for the synthesis of antibody-drug conjugates (ADCs)[1].

C-NH-Boc-C-Bis-(C-PEG1-Boc) is a versatile alkyl/ether-based PROTAC linker for synthesizing PROTACs[1].