VHN22300, also known as (S,R,S)-AHPC-PEG3-Alkyne, is a ProTAC building block. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand and a PEGylated crosslinker with pendant alkyne for click chemistry with an azide on the target ligand. When used with other protein degrader building blocks with a pendant alkyne group, parallel synthesis can be used to more quickly generate ProTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

(S,R,S)-AHPC-amido-C7-acid incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design PROTACs.

Pomalidomide-piperazine hydrochloride is an E3 ligase ligand-linker conjugate containing a CRBN-based ligand and linker, which can be used to synthesize PROTAC.

BWA-522 intermediate-1 is an intermediate in the synthesis of PROTAC BWA-522 (HY-149433) and serves as a ligand molecule for cereblon E3 ubiquitin ligase. BWA-522 is an orally active small molecule protein-targeting chimera (PROTAC) that has significant degradation effects on AR-FL and AR-V7.

Thalidomide-4-O-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide (HY-14658) based cereblon ligand and a linker used in PROTAC technology.

Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs[1]. Thalidomide-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Tri-GalNAc-DBCO is a PIP-GalNAc coupling compound that binds ASGPR to drive protein down-regulation and target compounds for protein degradation via copper-free strain-promoted azide-alkyne cycloaddition coupled to azide on a non-specifically labeled antibody.

M-MoDE-A (2) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).

D-MoDE-A (1) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).

Tri-GalNAc(OAc)3-Perfluorophenyl is a pentafluorophenyl modified Tri-GalNAc(OAc)3 (HY-148118), a tri-GalNAc ligand that can be used for the synthesis of GalNAc-LYTAC. GalNAc-LYTAC engages the asialoglycoprotein receptor for targeted protein degradation. tri-GalNAc: triantenerrary N-acetylgalactosamine; LYTAC: lysosome-targeting chimera.

tri-GalNAc-COOH acetylation is the acetylated and modified form of tri-GalNAc-COOH. tri-GalNAc-COOH acetylation can be used for the synthesis of LYTAC.

Tri-GalNAc(OAc)3 TFA is a tri-GalNAc ligand that can be used for the synthesis of GalNAc-LYTAC. GalNAc-LYTAC engages the asialoglycoprotein receptor for targeted protein degradation. tri-GalNAc: triantenerrary N-acetylgalactosamine; LYTAC: lysosome-targeting chimera.

Tri-GalNAc(OAc)3 is a triantenerrary N-acetylgalactosamine (tri-GalNAc) with an amino group, which is useful precursor for synthesis of GalNAc-LYTAC that engage the asialoglycoprotein receptor for targeted protein degradation. Tri-GalNAc(OAc)3 was first reported in Nat Chem Biol. 2021 Sep;17(9):937-946 (compound ). This product has no formal name at the moment.

tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.

Tri-GalNAc(OAc)3 Cbz is a ligand for asialoglycoprotein receptor (ASGPR) where the sugars are protected by acetylation and the tris tertiary amine is protected by benzyloxycarbonyloxy (Cbz). This peracetylated tri-GalNAc(OAc)3 Cbz can be serve as a valuable building block for ASGPR-targeted therapies. Its three branches or arms, each ending in a GalNAc sugar, ensure strong binding to hepatocyte ASGPR. However, the key feature lies in its protective groups: acetylated sugars allow for controlled removal to expose reactive sites for conjugation, while the Cbz-protected amine provides stability and can be selectively cleaved to introduce a reactive amine group for further biomolecule attachment, ultimately enabling researchers to tailor tri-GalNAc(OAc)3 Cbz into customized conjugates for specific therapeutic applications.

VRK-IN-1 is a potent and selective inhibitor of vaccinia-related kinases 1 (VRK1), with an IC50 of 150 nM. VRK1 is human Ser/Thr protein kinases associated with increased cell division and neurological disorders.

MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression.

PROTAC BTK Degrader-11 is a PROTAC degrader that can break down BTK, with a DC50 of 1.7 nM.

NIC3 is a selective nucleus accumbens-associated protein-1 (NAC1) inhibitor, binds to the conserved Leu-90 of NAC1, prevents its homodimerization, and leads to proteasomal NAC1 degradation. Anti-cancer activity

Lp(a)-IN-5 (Compound A) is an orally active lipoprotein (a) (Lp(a)) inhibitor. Lp(a)-IN-5 inhibits the assembly of Apo(a) and ApoB proteins with an IC50 value of 0.41 nM. Lp(a)-IN-5 is promising for research of diseases related to elevated plasma Lp(a) levels, such as cardiovascular diseases.

BRD-810 is a potent and selective MCL1 inhibitor with Kd of 0.3 nM (SPR) and IC50 of 0.4 nM (MCL1-Noxa HTRF), respectively. BRD-810 is a rapidly cleared inhibitor of MCL1 that has robust antitumor efficacy in hematological and solid tumor cancer models.

ALG-055009 is a potent and selective thyroid hormone receptor beta (THR-β) agonist with EC50 of 0.063 μM. ALG-055009 is highly metabolically stable, with good permeability and a relatively low efflux ratio.

Vicadrostat (compound 29 A) is a potent and selective inhibitor of aldosterone synthase(CYP11B2) with an IC50 of 16 nM. It exhibits potential in renal disease, diabetic nephropathy, cardiovascular diseases and fibrotic disorder research.

Risvodetinib is a potent protein tyrosine kinase inhibitor. Risvodetinib involves in synthesis of Abelson protein kinases (c-Abl1, c-Abl2, and c-kit) inhibitor.

Barbadin is a small molecule that selectively inhibits the β-arrestin/β2-adaptin interaction (IC50=19.1/15.6 uM for β-arrestin1/2) without effect on the formation of receptor/β-arrestin complexes.

Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively.

TCMDC-136364 (AKT Kinase Inhibitor) is an Akt kinase inhibitor, selectively inhibits Akt in proliferating cells expressing Trop-2, also potently inhibits P. falciparum multidrug resistant strain Dd2.

dTAGV-1 hydrochloride is a potent and selective degrader of FKBP12F36V-tagged proteins PROTAC degrader. dTAGV-1 hydrochloride can induce degradation of FKBP12F36V-Nluc in vivo.