Ligand for E3 Ligase

(S,R,S)-AHPC is a VHL ligand that used in the recruitment of the VHL protein.

Lenalidomide-Br is an analog of the cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, which is used in the recruitment of CRBN proteins. It is able to utilize linkers to attach to protein ligands to form PROTACs such as the PROTAC STAT3 degrader SD-36.

Pomalidomide-PEG4-C2-NH2 (E3 Ligase Ligand-Linker Conjugates 22) is a synthesized E3 ligase ligand-linker conjugate incorporating the Pomalidomide-based cereblon ligand and 4-unit PEG linker.

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.

(S,R,S)-AHPC TFA (VHL ligand 1 TFA) (VH032-NH2 TFA) is a VH032-based ligand designed for von Hippel-Lindau (VHL) protein recruitment. This compound can be linked to protein ligands (e.g., BCR-ABL1) using a linker to create PROTACs (e.g., GMB-475), which effectively induce the degradation of BCR-ABL1, demonstrated by an IC50 of 1.11 μM in Ba/F3 cells.

(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate, comprising the (S,R,S)-AHPC-based VHL ligand and a linker, designed for BET-targeted PROTAC applications.

(S,R,S)-AHPC-Me-C10-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating a VHL ligand and a linker.

VH032 commonly used as a precursor to a PROTAC that hijacks VHL as the E3 ubiquitin ligase component.VH032 is a VHL/HIF-1α interaction inhibitor with a KdPROTACs, which can recruit von Hippel-Lindau (VHL) proteins as a ligand of VHL.

E3 ligase Ligand 23 is a cereblon binding agent that degrades Ikaros or Aiolos via the ubiquitin proteasome.

VH-298 is a potent inhibitor of VHL that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes.

Thalidomide (Thalomid) is a synthetic derivative of glutamic acid (alpha-phthalimido-glutarimide) with teratogenic, immunomodulatory, anti-inflammatory and anti-angiogenic properties.

Pomalidomide (CC-4047) inhibits TNF-α release in LPS stimulated human PBMCs (IC50: 13 nM). It is an anti-angiogenic agent and an immunomodulator.

Lenalidomide (CC-5013) is a potent inhibitor of TNF-α that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines.

Thalidomide-O-amido-PEG3-C2-NH2 TFA (Cereblon Ligand-Linker Conjugates 3 (TFA)) is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-PEG3-C2-NH2 TFA incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.

Thalidomide-NH-C4-NH-Boc is a synthesized conjugate used in PROTAC technology, combining a Thalidomide-based cereblon ligand with a linker.

Thalidomide 5-fluoride (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-fluoro-) is a thalidomide-based Cereblon ligand that binds to the IRAK4 protein ligand via a linker to form PROTACIRAK4 degrader-1.

(S,R,S)-AHPC-PEG2-NH2 dihydrochloride (VH032-linker 12) is a synthesized E3 ligase ligand-linker conjugate incorporating the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker[1].

(S,R,S)-AHPC-C4-NH2 hydrochloride (E3 ligase Ligand-Linker Conjugates 28) is a synthesized E3 ligase ligand-linker conjugate incorporating the (S,R,S)-AHPC based VHL ligand and a linker.

Thalidomide-O-amido-C3-NH2 TFA (Cereblon Ligand-Linker Conjugates 16 TFA) is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-C3-NH2 TFA incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

Lenalidomide-OH is an analog of Lenalidomide, a cereblon ligand for E3 ubiquitin ligase (CRBN), used for CRBN protein recruitment. It is able to attach to protein ligands using linkers to form PROTAC.

Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride incorporates an E3 ligase ligand and a linker. Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride can be used as an immunomodulator for the treatment of cancer.

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is a chemical compound utilized in the synthesis of ARV-771, an exceptionally potent BET protein degrader. This compound selectively degrades BET protein in cells resistant to castration, exhibiting a remarkable DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, (S,R,S)-AHPC-Me hydrochloride serves as the VHL ligand derived from (S,R,S)-AHPC for the recruitment of von Hippel-Lindau (VHL) protein.

Thalidomide-5-methyl is the Thalidomide-based cereblon (CRBN) ligand. Thalidomide-5-methyl is used in the recruitment of CRBN protein.

Thalidomide-5-OH (2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione) is the Thalidomide-based cereblon ligand that used in the recruitment of CRBN protein. It can be connected to the ligand for protein by a linker to form PROTAC.

VL285 is a potent VHL ligand, degrading HaloTag7 fusion proteins.

Pomalidomide-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate. Pomalidomide-C2-NH2 hydrochloride incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.

Thalidomide-4-OH (E3 ligase Ligand 2) (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used to recruit of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) is a linker to form PROTACs

(S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-linker 10) is a synthesized E3 ligase ligand-linker conjugate incorporating the (S,R,S)-AHPC based VHL ligand and a linker[1].

Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. It can be connected to the ligand for protein by a linker to form PROTACs.

Pomalidomide-C2-NH2 (4-[(2-Aminoethyl)amino]-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione) is a synthesized E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand and a linker.

(S,R,S)-AHPC-Me is a VHL ligand based on (S,R,S)-AHPC that can be used to recruit von Hippel-Lindau (VHL) proteins. It efficiently degrades BET proteins in desmoplasia-resistant prostate cancer cells with a DC50 < 1 nM, and it can be used to synthesize ARV-771.

CRBN modulator-1 (WUN29654) is a Thalidomide analog and CRBN modulator,has an IC50 of 3.5 μM and a Ki of 0.98 μM.

VH032-cyclopropane-F is a VHL ligand based on VH032. It is able to utilize linkers to ligands of target proteins to yield PROTAC molecules such as PROTAC 1. PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4.

(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC is potential useful for the targeted degradation of the androgen receptor.

SMER3 is an inhibitor of the Skp1-Cullin-F-box (SCF)(Met30) ubiquitin ligase, a member of the SCF E3-ligase family, which regulates diverse cellular processes including transcription, cell-cycle control and immune response.

(S, R, S)-AHPC-PEG3-N3 (VHL Ligand-Linker Conjugates 8) is a synthesized E3 ligase ligand-linker conjugate. (S, R, S)-AHPC-PEG3-N3 incorporates the (S, R, S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.

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

Thalidomide 4-fluoride (E3 ligase Ligand 4) (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand. Thalidomide 4-fluoride can be used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.

LS-102 is a selective inhibitor of the E3 ligase synoviolin (Syvn1), an astragaloside IV derivative, which attenuates myocardial ischemia/reperfusion injury by inhibiting mitochondrial fission.LS-102 inhibits Syvn1 auto-ubiquitylation, which ameliorates amyloidazole-induced slowing of the heart rate, and is useful for studying cardiovascular diseases.

CC-885 is a modulator of cereblon (CRBN). It has potent anti-tumour activity.

Pomalidomide-PEG4-Ph-NH2 is a synthetic E3 ligase ligand-linker conjugate combining a Pomalidomide-based cereblon ligand and a 4-unit PEG linker.

HaloPROTAC3 (HaloPROTAC-3) is a conjugate of ligands for E3 and 16-atom-length linker and a degrader of HaloTag fusion proteins.

Thalidomide-O-amido-C4-N3 (Cereblon Ligand-Linker Conjugates 4) is an E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and a linker.

CRBN ligand-9 (2-(2,6-dioxopiperidin-3-yl)-5-nitroisoindoline-1,3-dione) exhibit inhibition of CRBN.

Dicyclanil is an insect growth regulator with a chemical structure similar to that of cyclopromazine.

Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).

5-Aminothalidomide is a E3 ligase ligand used in PROTAC technology.

CFT7455 (Cemsidomide) is an anti-cancer agent showing high affinity to the cereblon E3 ligase with a Kd of 0.9 nM. CFT7455 is an orally active degrader of zinc finger transcription factors Ikaros (IKZF1), and Aiolos (IKZF3).

(S,R,S)-AHPC-PEG4-NH2 (VHL Ligand-Linker Conjugates 4) is a synthetic E3 ligase ligand-linker conjugate comprising a VHL ligand based on (S,R,S)-AHPC and a 4-unit PEG linker.

(S,S,S)-AHPC hydrochloride is a von Hippel-Lindau (VHL) aminoblock. (S,S,S)-AHPC (Compound 27) is often used as a negative control for (S,R,S)-AHPC. (S,R,S)-AHPC is a VHL ligand based on VH032 and can be used to recruit VHL proteins.