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PROTACMolecular Glues
Molecular glue refers to a class of chemical compounds or molecules that play a crucial role in binding and stabilizing protein-protein interactions in biological systems. These molecules act as "glue" by enhancing the affinity between proteins, ultimately influencing various cellular processes. Molecular glue compounds have gained significant attention in the fields of drug discovery, chemical biology, and fundamental research due to their potential to modulate protein interactions, and thus, impact various cellular pathways. They have unlocked avenues in medicine previously thought to be “undruggable.”
KT-333
T883582502186-79-8
KT-333 is a potent, highly selective, heterobifunctional small molecule degrader of STAT3 for the treatment of a variety of STAT3-dependent pathologies, including hematologic malignancies and solid tumors.KT-333 specifically binds to STAT3 proteins at one end of the spectrum, and binds to the E3 ubiquitin ligase, VHL, at the other end.
- $413
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Golcadomide
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
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Iberdomide
Cited
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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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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CitedJasmonic acid
T1243846894-38-8
Jasmonic acid (JA) is a phytohormone and plant growth regulator involved in plant defense and growth and development.Jasmonic acid plays an important role in signaling, inducing the MAP kinase cascade pathway and calcium channels.
- $196
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E7820
T4435289483-69-8
E7820 (ER68203-00) is an angiogenesis inhibitor by suppressing integrin a2 (a cell adhesion molecule expressed on endothelial cells).
- $30
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Lenalidomide Cited
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
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Cited
T2017993050683-29-6
VAV1 degrader-2 (Example 176) is a molecular gel degrader (DC50=4.41 nM) that targets VAV 1 for the study of inflammatory and autoimmune diseases.
- $226
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Indisulam Cited
T4321165668-41-7
Indisulam (E 7070) is a carbonic anhydrase inhibitor and antitumor CDK inhibitor that targets the G1 phase of the cell cycle by depleting cyclin E, inducing p53 and p21, and inhibiting CDK2, thereby causing a blockade in the G1/S transition.
- $30
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CitedVAV1 degrader-3
T2013923050683-38-7
VAV1 degrader-3 is an orally active and efficient VAV1 molecular glue degrader that reduces immune cell activation, proliferation, and cytokine production, useful for studying inflammation and autoimmune diseases.
- $596
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NRX-252114
T635162763260-39-3In house
NRX-252114 (NRX252114) induces degradation of mutant β-catenin NRX-252114 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP, and is able to enhance the binding of pSer33/S37A β-catenin to β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. Kd is 0.4 nM.
- $196
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3-Indoleacetic acid Cited
T2O279187-51-4
3-Indoleacetic acid (indolylacetic acid) (IAA) is the most common plant hormone of the auxin class and it regulates various aspects of plant growth and development.
- $41
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CitedMezigdomide
T107032259648-80-9In house
Mezigdomide (CC-92480) is a potent, novel, selective and active cereblon E3 ubiquitin ligase modulator (CELMoD) that acts as a molecular glue. Mezigdomide has anti-myeloma activity. [1]
- $118
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Pomalidomide Cited
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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CitedEragidomide
T107651860875-51-9
Dicyclanil is an insect growth regulator with a chemical structure similar to that of cyclopromazine.
- $34
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BI-3802
T54082166387-65-9
BI-3802, a highly potent BCL6 degrader, targets and inhibits the Bric-à-brac (BTB) domain of BCL6, exhibiting an IC50 value of ≤3 nM. It induces polymerization of BCL6 and facilitates its degradation in a manner dependent on the E3 ligase SIAH1, demonstrating notable antitumor activity[1][2].
- $127
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(R)-CR8
T12617L294646-77-8
(R)-CR8 ((R)-Isomer) is a potent and selective CDK inhibitor.
- $61
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Thalidomide Cited
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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CitedNRX-103094
T634272763260-36-0In house
NRX-103094 is a potent enhancer of the interaction between β-catenin and the homologous E3 ligase SCFβ-TrCP, increasing the affinity of pSer33/Ser37 β-catenin for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM.
- $67
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Avadomide Cited
T35491015474-32-4
Avadomide (CC 122) is an orally available pleiotropic pathway modulator with potential antineoplastic activity.
- $40
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CitedLL-K12-18
T89229
LL-K12-18 is a dual-site molecular gel that enhances protein-protein interactions (PPIs) between CDK12-DDB1 complexes thereby promoting the degradation of Cyclin K. It potently inhibits tumor cell gene transcription and anti-proliferation.
- $148
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Voclosporin
T17235515814-01-4
Voclosporin (ISAtx-247) is a novel, orally available calcium-modulated phosphatase (CN; PP2B) inhibitor and immunosuppressant used for treating lupus nephritis.
- $106
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Chloroquinoxaline sulfonamide
T1495397919-22-7In house
Chloroquinoxaline sulfonamide (Chloroquinoxaline) is a topoisomerase II alpha/beta toxin with antitumor activity and immunosuppressive properties that inhibits the proliferation of B16 melanoma cells in mice, and can be used to study metastatic colorectal cancer. It can be used to study metastatic colorectal cancer.
- $56
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