9decyn1ol

9-Decyn-1-ol is an alkyl ether-based PROTAC linker used in synthesizing PROTACs, acting as a conjugation agent to combine GDC-0068 and Lenalidomide to form INY-03-041. INY-03-041 is a potent and highly selective pan-Akt degrader that inhibits Akt1, Akt2, and Akt3 with IC50 values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively[1].

PROTAC CDK2 9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).

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

PROTAC BRD9-binding moiety 1 that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.

PROTAC BRD9-binding moiety 1 hydrochloride inhibits BRD9 activity by binding to BRD9, utilizing the PROTAC (Proteolysis Targeting Chimera) mechanism.

Azido-PEG9-amine, a non-cleavable 9-unit PEG ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs)[1].

NH2-PEG9-acid is a non-cleavable 9 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7 9 inhibitor), interacts with a VHL ligand via a linker to form the PROTAC VZ185 (targeting BRD7 9 with DC50 values of 4.5 and 1.8 nM, respectively)[1].

BRD7-IN-1, a modified derivative of BI7273 (BRD7 9 inhibitor), forms PROTAC VZ185 via linkage to a VHL ligand, demonstrating potent activity against BRD7 9 with DC50 values of 4.5 and 1.8 nM, respectively [1].

E3 ligase Ligand 9 is a compound that acts as a ligand for E3 ubiquitin ligase and can be attached to a protein ligand via a linker to form PROTACs or SNIPERs, which degrade cancer-promoting proteins through ubiquitination-mediated mechanisms[1].

cIAP1 Ligand-Linker Conjugates 2 Hydrochloride is a chemical compound that combines an IAP ligand, targeting the E3 ubiquitin ligase, with a PROTAC linker and is utilized in the creation of SNIPERs[1].

cIAP1 Ligand-Linker Conjugates 9 feature an IAP ligand specifically targeting the E3 ubiquitin ligase, along with a PROTAC linker. It is valuable tools for developing SNIPERs[1].

(S,R,S)-AHPC-PEG1-N3 (E3 ligase Ligand-Linker Conjugates 3) is a synthesized E3 ligase ligand-linker conjugate that includes the (S,R,S)-AHPC-based VHL ligand and a 1-unit PEG linker used in PROTAC technology.

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.

NH2-C2-amido-C2-Boc is an alkyl ether-based PROTAC linker used in synthesizing various PROTACs, including PROTAC CDK2 9 Degrader-1[1]. NH2-C5-NH-Boc also serves as a suitable precursor for synthesizing these PROTACs.

Thalidomide-C2-amido-C2-COOH is a compound that includes a CRBN ligand for the E3 ubiquitin ligase, as well as a linker. It is utilized in the development of PROTAC CDK2 9 Degrader-1[1].

JQ dS-4 is a degrader of Brahma-related gene 1 (BRG1) BRM SMARCA4 (PROTAC®; DC50 range = 9 - 390 nM in glioma models and cell lines), featuring a BRG1 inhibitor connected through a linker to a cereblon (CRBN) E3 ligase ligand. It effectively degrades BRG1 completely over 48 and 72 hours in HSJD-DIPG007 and SU-DIPGXIIIP cells. Additionally, it lessens the viability of various cancer cell lines, including those of H3K27M glioma, prostate, thyroid, and salivary gland.

ROR1ligand-1 (9-1) serves as the ligand for PROTAC ROR1 degrader-1. By linking with ligands of either the VHL type or CRBN, the first selective and efficient ROR1 PROTAC molecule was designed and synthesized.

PROTAC FGFR1 degrader-1 (compound S2H) is a targeted degrader of FGFR1, demonstrating an IC50 of 26.81 nM and a DC50 of 39.78 nM in KG1a cells. This compound is composed of a CRBN-type E3 ligase ligand (blue part) Pomalidomide, a target protein ligand (red part) FGFR1ligand-1, and a PROTAC linker (black part) 9-Bromononanoic acid, together forming the conjugate E3LigaseLigand-linker Conjugate 164.

CDK9 Antagonist-1 (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]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

PROTAC CDK9 ligand-1, a CDK9 ligand, is used in the synthesis of PROTACs.

PROTAC CDK9 Degrader-1 is a selective PROTAC CDK9 degrader composed of a cereblon ligand and a CDK9 ligand.

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].

PROTAC pan-IAP degrader-1 (Compound 9) is a pan- IAP degrader PROTAC . PROTAC pan-IAP degrader-1 degrades XIAP , cIAP1 and cIAP2 with DC 50 s of 0.7, 2.4, and 6.2 nM in MM.1S cells, respectively [1] .