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PROTACLigand for E3 Ligase
A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to be degraded via the ubiquitin–proteasome system. The advent of nonpeptidic small-molecule E3 ligase ligands, notably for von Hippel–Lindau (VHL) and cereblon (CRBN), revolutionized the field and ushered in the design of drug-like PROTACs with potent and selective degradation activity.
- HaloPROTAC3T320431799506-07-2HaloPROTAC3 (HaloPROTAC-3) is a conjugate of ligands for E3 and 16-atom-length linker and a degrader of HaloTag fusion proteins.
- $112
SizeQTY - LenalidomideT1642191732-72-6Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.
- $36
SizeQTY
Cited - (S,R,S)-AHPC hydrochlorideT42071448189-80-7(S,R,S)-AHPC hydrochloride (Protein degrader 1 hydrochloride) is a building block in the synthesis of proteolysis-targeting chimera technologies (PROTACs).
- $48
SizeQTY - PomalidomideT238419171-19-8Pomalidomide (CC-4047) is an anti-angiogenic and immunomodulatory agent. Pomalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN) and is commonly used in the synthesis of PROTAC products.
- $52
SizeQTY Cited - IberdomideT77911323403-33-3Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).
- $39
SizeQTY
- (S,R,S)-AHPC-PEG1-N3T179202101200-09-1(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.
- $33
SizeQTY - (S,R,S)-AHPC-PEG3-N3T179091797406-80-4(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.
- $37
SizeQTY - AvadomideT35491015474-32-4Avadomide (CC 122) is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
- $34
SizeQTY - (S,S,S)-AHPC hydrochlorideT138772115897-23-7(S,S,S)-AHPC hydrochloride ((S,S,S)-VH032-NH2 hydrochloride) is a VHL amino building block and ligand used as a negative control for (S,R,S)-AHPC. It is based on VH032 and is employed in the recruitment of the VHL protein.
- $40
SizeQTY - EragidomideT107651860875-51-9Dicyclanil is an insect growth regulator with a chemical structure similar to that of cyclopromazine.
- $34
SizeQTY - CFT7455T600242504235-67-8CFT7455 (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).
- $79
SizeQTY - VH032T291061448188-62-2In houseVH032 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.
- $44
SizeQTY - CC-885T148931010100-07-8CC-885 is a modulator of cereblon (CRBN). It has potent anti-tumour activity.
- $51
SizeQTY - ThalidomideT021350-35-1Thalidomide (Thalomid) is a synthetic derivative of glutamic acid (alpha-phthalimido-glutarimide) with teratogenic, immunomodulatory, anti-inflammatory and anti-angiogenic properties.
- $50
SizeQTY Cited - BC-1215T58211507370-20-8BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg mL for IL-1β release).
- $47
SizeQTY - GolcadomideT637712379572-34-4Golcadomide (CC-99282) is a orally active CRBN E3 ligase modulator that induces interactions between CRBN and its neo-substrate, recruiting the target disease-causing proteins and the E3 ubiquitin ligase.Golcadomide is used in the study of hematologic malignancies.
- $165
SizeQTY - VH-298TQ01212097381-85-4VH-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.
- $39
SizeQTY Cited - Thalidomide-O-amido-C4-N3T151892098488-36-7Thalidomide-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.
- $51
SizeQTY - (S,R,S)-AHPC-C10-NH2T178812341796-74-3(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate, comprising an (S,R,S)-AHPC-based VHL ligand and a linker, designed for BET-targeted PROTAC applications.
- $51
SizeQTY - (S,R,S)-AHPC-PEG2-N3T179132010159-45-0(S,R,S)-AHPC-PEG2-N3 (VHL Ligand-Linker Conjugates 6) is a synthesized E3 ligase ligand-linker conjugate comprising a (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker.
- $33
SizeQTY - Thalidomide-O-amido-C6-NH2 TFAT179191950635-14-9Thalidomide-O-amido-C6-NH2 TFA (Cereblon Ligand-Linker Conjugates 11 TFA) is a synthesized E3 ligase ligand-linker conjugate comprising a Thalidomide-based cereblon ligand and a linker.
- $33
SizeQTY - LS-102T118791456891-34-1LS-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.
- $39
SizeQTY - (S,R,S)-AHPCT400282055344-67-5(S,R,S)-AHPC is a VHL ligand that used in the recruitment of the VHL protein.
- $59
SizeQTY - (S,R,S)-AHPCT84121448297-52-6(S,R,S)-AHPC (VH032-NH2) is a VH032-based ligand for recruiting the von Hippel-Lindau (VHL) protein, potentially useful for the targeted degradation of the androgen receptor.
- $59
SizeQTY - (S,R,S)-AHPC TFAT179271631137-51-3(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.
- $30
SizeQTY - CRBN modulator-1T88242407829-65-4CRBN modulator-1 (WUN29654) is a Thalidomide analog and CRBN modulator,has an IC50 of 3.5 μM and a Ki of 0.98 μM.
- $33
SizeQTY - Lenalidomide hemihydrateT22922847871-99-2Lenalidomide hemihydrate is a derivative of Thalidomide, an orally active immunomodulator that acts as a molecular gel. It is a ligand for the ubiquitin E3 ligase cereblon, which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase.
- $29
SizeQTY - Thalidomide 5-fluorideT9381835616-61-0Thalidomide 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.
- $29
SizeQTY - Thalidomide 4-fluorideT7755835616-60-9Thalidomide 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.
- $29
SizeQTY - Thalidomide-4-OHT77635054-59-1Thalidomide-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
- $29
SizeQTY - Thalidomide-5-OHT929164567-60-8Thalidomide-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.
- $29
SizeQTY - Lenalidomide-BrT180642093387-36-9Lenalidomide-Br (Compound 41), a derivative of Lenalidomide, acts as a ligand for cereblon (CRBN) - an E3 ubiquitin ligase involved in protein recruitment. This compound can be conjugated to a protein ligand via a linker to create PROTACs, such as the PROTAC STAT3 degrader SD-36.
- $29
SizeQTY - 5-AminothalidomideT40017191732-76-05-Aminothalidomide is a E3 ligase ligand used in PROTAC technology.
- $39
SizeQTY - Pomalidomide-PEG4-C2-NH2T179162225940-52-1Pomalidomide-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.
- $30
SizeQTY - Thalidomide-5-methylT4050340313-92-6Thalidomide-5-methyl is a Thalidomide-based cereblon (CRBN) ligand used for the recruitment of CRBN protein.
- $117
SizeQTY - AR antagonist 1T103591818885-54-9AR 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.
- $78
SizeQTY - (S,R,S)-AHPC-Me-C10-NH2 hydrochlorideT18669L2471970-07-5(S,R,S)-AHPC-Me-C10-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating a VHL ligand and a linker.
- $89
SizeQTY - E3 ligase Ligand 23T9809444287-56-3In houseE3 ligase Ligand 23 is a cereblon binding agent that degrades Ikaros or Aiolos via the ubiquitin proteasome.
- $31
SizeQTY - Thalidomide-O-amido-PEG3-C2-NH2 TFAT77581957236-21-3Thalidomide-O-amido-PEG3-C2-NH2 TFA (Cereblon Ligand-Linker Conjugates 3 (TFA)) is a synthesized E3 ligase ligand-linker conjugate incorporating a Thalidomide-based cereblon ligand and a 3-unit PEG linker, used in PROTAC technology.
- $33
SizeQTY - (S,R,S)-AHPC-PEG2-NH2 dihydrochlorideT186752341796-76-5(S,R,S)-AHPC-PEG2-NH2 dihydrochloride (VH032-linker 12) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker[1].
- $34
SizeQTY - Thalidomide-NH-C4-NH-BocT188072093388-52-2Thalidomide-NH-C4-NH-Boc is a synthesized conjugate used in PROTAC technology, combining a Thalidomide-based cereblon ligand with a linker.
- $30
SizeQTY - SMER3T2337167200-34-4SMER3 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.
- $29
SizeQTY - VH032-cyclopropane-FT178772306193-99-5VH032-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.
- $39
SizeQTY - (S,R,S)-AHPC-C4-NH2 hydrochlorideT186402245697-83-8(S,R,S)-AHPC-C4-NH2 hydrochloride (E3 ligase Ligand-Linker Conjugates 28) is a synthesized E3 ligase ligand-linker conjugate comprising the (S,R,S)-AHPC-based VHL ligand and a linker.
- $32
SizeQTY - Thalidomide-O-amido-PEG2-C2-NH2 hydrochlorideT188192376990-30-4Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride, incorporating an E3 ligase ligand and a linker, can be used as an immunomodulator for the treatment of cancer.
- $30
SizeQTY - Thalidomide-O-amido-C3-NH2 TFAT77602022182-58-5Thalidomide-O-amido-C3-NH2 TFA (Cereblon Ligand-Linker Conjugates 16 TFA) is a synthesized E3 ligase ligand-linker conjugate incorporating a Thalidomide-based cereblon ligand and a linker used in PROTAC technology.
- $30
SizeQTY - (S,R,S)-AHPC-Me hydrochlorideT136711948273-03-7(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is utilized in the synthesis of ARV-771, a potent BET protein degrader. It selectively degrades BET protein in castration-resistant cells with a DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, it serves as the VHL ligand from (S,R,S)-AHPC for recruiting von Hippel-Lindau (VHL) protein.
- $34
SizeQTY - Lenalidomide-OHT180661416990-08-3Lenalidomide-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.
- $42
SizeQTY - Pomalidomide-C2-NH2 hydrochlorideT77612305369-00-8Pomalidomide-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating the Pomalidomide-based cereblon ligand and a linker used in [PROTAC] technology.
- $31
SizeQTY - Pomalidomide-PEG4-Ph-NH2T77561818885-63-0Pomalidomide-PEG4-Ph-NH2 is a synthetic E3 ligase ligand-linker conjugate that integrates a Pomalidomide-based cereblon ligand with a 4-unit PEG linker.
- $30
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