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PROTACLigands for E3 Ligase
E3 ligands are an important part of PROTAC (proteolytic targeting chimeric molecule), which together with target protein ligands and linkers constitute PROTAC molecule. It can be a derivative structure of an endogenous ligand peptide segment, or it can be a small molecule compound. Common E3 ligands include CRBN, VHL, IAP and MDM2.
Golcadomide
CC-99282, CC99282, CC 99282
T637712379572-34-4
Golcadomide (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
Size
QTY
HaloPROTAC3
HaloPROTAC-3, HaloPROTAC 3, Halo PROTAC-3
T320431799506-07-2
HaloPROTAC3 (HaloPROTAC-3) is a conjugate of ligands for E3 and 16-atom-length linker and a degrader of HaloTag fusion proteins.
- $112
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QTY
Iberdomide
Cited
CC-220
T77911323403-33-3
Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).
- $39
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QTY
CitedCC-885 Cited
T148931010100-07-8
CC-885 is a modulator of cereblon (CRBN). It has potent anti-tumour activity.
- $51
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QTY
CitedLenalidomide Cited
CC-5013
T1642191732-72-6
Lenalidomide (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
Size
QTY
CitedCFT7455 Cited
Cemsidomide
T600242504235-67-8
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).
- $79
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QTY
CitedcIAP1 ligand 1
E3 ligase Ligand 12
T178702095244-42-9
cIAP1 ligand 1 (E3 ligase Ligand 12) is an apoptotic protein ligand based on the LCL161 derivative that recruits IAP ubiquitin ligases to degrade target proteins, and can be used in conjunction with androgen receptor ligands for the development of protein degradation agents that can be used in the study of prostate cancer.
- $42
Size
QTY
Pomalidomide Cited
CC-4047
T238419171-19-8
Pomalidomide (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
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QTY
CitedEragidomide
Cereblon modulator 1, CC-90009
T107651860875-51-9
Dicyclanil is an insect growth regulator with a chemical structure similar to that of cyclopromazine.
- $34
Size
QTY
(S,R,S,R)-AHPC-Me
T400282055344-67-5
(S,R,S,R)-AHPC-Me is a VHL ligand that used in the recruitment of the VHL protein.
- $36
Size
QTY
TFC-007
TFC007
T24870927878-49-7
TFC-007 is a selective and efficient hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, suppressing inflammatory factors. It can be used to synthesize H-PGDS degrader PROTAC (H-PGDS)-1 and study cedar pollen-induced guinea pig allergic rhinitis.
- $64
Size
QTY
(S,R,S)-AHPC-Me
VHL ligand 2, E3 ligase Ligand 1A
T77521948273-02-6
(S,R,S)-AHPC-Me (E3 ligase Ligand 1A) (VHL ligand 2) is an (S,R,S)-AHPC-based VHL ligand used to recruit the von Hippel-Lindau (VHL) protein. It is utilized in the synthesis of ARV-771, a VHL E3 ligase-based BET PROTAC degrader that effectively degrades BET proteins in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
- $31
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QTY
(S,R,S)-AHPC hydrochloride
VHL Ligand 1 hydrochloride, ULM-1, Protein degrader 1 hydrochloride
T42071448189-80-7
(S,R,S)-AHPC hydrochloride (Protein degrader 1 hydrochloride) is a building block in the synthesis of proteolysis-targeting chimera technologies (PROTACs).
- $33
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QTY
(S,R,S)-AHPC-Me-C10-NH2 hydrochloride
T18669L2471970-07-5
(S,R,S)-AHPC-Me-C10-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating a VHL ligand and a linker.
- $89
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QTY
Thalidomide Cited
Thalomid, Sedoval
T021350-35-1
Thalidomide (Thalomid) is a synthetic derivative of glutamic acid (alpha-phthalimido-glutarimide) with teratogenic, immunomodulatory, anti-inflammatory and anti-angiogenic properties.
- $50
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QTY
CitedAvadomide Cited
CC 122
T35491015474-32-4
Avadomide (CC 122) is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
- $40
Size
QTY
Cited(S,R,S)-AHPC-PEG4-NH2
VHL Ligand-Linker Conjugates 4, VH032-PEG4-NH2, E3 ligase Ligand-Linker Conjugates 7 Free Base
T15190L2010159-57-4
(S,R,S)-AHPC-PEG4-NH2 (VHL Ligand-Linker Conjugates 4) is a synthetic E3 ligase ligand-linker conjugate, consisting of a VHL ligand based on (S,R,S)-AHPC combined with a 4-unit PEG linker.
- $40
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QTY
VH032 Cited
VH-032, VH 032
T291061448188-62-2In house
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.
- $40
Size
QTY
CitedPomalidomide-C2-NH2 hydrochloride
T77612305369-00-8
Pomalidomide-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating the Pomalidomide-based cereblon ligand and a linker used in [PROTAC] technology.
- $49
Size
QTY
(S)-Thalidomide
(S)-(-)-Thalidomide
T12644L841-67-8In house
(S)-Thalidomide ((S)-(-)-Thalidomide) is the S-isomer of Thalidomide with immunomodulatory, anti-inflammatory, anticancer, anti-angiogenic, and pro-apoptotic activities, used in studying leprosy erythema nodosum and myeloma.
- $56
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QTY
Thalidomide-O-amido-PEG2-C2-NH2 hydrochloride
T188192376990-30-4
Thalidomide-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.
- $32
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QTY
ZXH-1-161
T630102407654-51-5
ZXH-1-161 is a potent Cereblon (CRBN) modulator PROTAC that selectively degrades GSPT1 for use in multiple myeloma research.
- $1,490
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QTY
Lenalidomide hemihydrate
T22922847871-99-2
Lenalidomide 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
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Thalidomide-O-amido-C4-N3
E3 ligase Ligand-Linker Conjugates 18, Cereblon Ligand-Linker Conjugates 4
T151892098488-36-7
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.
- $35
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