JP-2-249 functions as a molecular glue degrader that selectively targets SMARCA2 for proteasomal degradation. In MV-4-11 leukemia cells, treatment with JP-2-249 (1–10 μM) induces dose-dependent reduction of SMARCA2 protein levels, demonstrating potent degradation activity.

PLX-4545 is an orally bioavailable molecular glue degrader that hijacks the cereblon E3 ubiquitin ligase complex to selectively target IKZF2 (Helios), a zinc finger transcription factor critical for regulatory T cell (Treg) function. By inducing proteasomal degradation of IKZF2, PLX-4545 disrupts Treg stability and reprograms these immunosuppressive cells into pro-inflammatory effector-like T cells, effectively shifting the tumor microenvironment toward immune activation.

CC-3240 is an optimized molecular glue degrader derived from ​CC-8977, demonstrating high-affinity binding to ​CaMKK2 (IC50 = 9 nM) and potent degradation efficacy (DC50 = 100 nM in THP1 cells, Dmax = 92%). This novel compound effectively hijacks the ubiquitin-proteasome system to induce ​targeted CaMKK2 depletion, offering a superior pharmacological approach over traditional kinase inhibition.

dCK1α-2 is an orally bioavailable molecular glue degrader targeting CK1α, a key regulator of p53 pathway signaling. This compound demonstrates robust in vivo anti-tumor activity in murine models while upregulating expression of p53-associated genes, highlighting its dual mechanism of action.

(R)-CR8 (CR8), a second-generation derivative of Roscovitine, is a highly effective inhibitor of CDK1/2/5/7/9. It exhibits inhibitory activity against CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM), and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and demonstrates neuroprotective properties. Additionally, it functions as a molecular glue degrader, specifically targeting and depleting cyclin K.

MMH2 is a novel BRD4 molecular glue degrader that operates by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2).

MMH1 is a first-in-class molecular glue degrader that specifically targets the second bromodomain of BRD4 (BRD4BD2) through an innovative mechanism of action. By simultaneously engaging both BRD4BD2 and the CUL4-DCAF16 E3 ubiquitin ligase complex, MMH1 induces targeted protein degradation with exceptional specificity.

TMX1 is a covalent molecular glue degrader targeting BRD4. It selectively recruits DCAF16 to the BRD4BD2 domain, resulting in the degradation of BRD4.

HQ461 is a molecular glue degrader that facilitates the interaction between CDK12 and the DDB1-CUL4-RBX1 E3 ubiquitin ligase, resulting in the polyubiquitination and subsequent degradation of the CDK12-interacting protein Cyclin K (CCNK). This degradation impairs CDK12 function, leading to reduced phosphorylation of its substrates, downregulation of DNA damage response genes, and ultimately, cell death.

EN450 is a cysteine-reactive covalent molecular glue degrader specifically designed to target NF-κB.

HQ005 is a highly efficient molecular glue degrader that induces the selective degradation of ​Cyclin K (CCNK) with exceptional potency (DC50 = 41 nM). By facilitating novel protein-protein interactions between ​CCNK and the ​ubiquitin-proteasome system, HQ005 promotes targeted ubiquitination and proteasomal clearance of CCNK, offering a precise pharmacological tool for modulating ​CDK12/13-dependent transcription and ​DNA damage response pathways.

dCeMM2 (Compound 2) is a molecular glue degrader that drives the ubiquitination and degradation of cyclin K. It achieves this by facilitating an interaction between the CDK12-cyclin K complex and the CRL4B ligase complex.

WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active molecular glue degrader targeting c-Myc. It facilitates the degradation of c-Myc through the ubiquitin E3 ligase CHIP-mediated 26S proteasome pathway. WBC100 is specifically utilized for research involving c-Myc overexpressing tumors.

dCeMM1 is a molecular glue degrader targeting RBM39. It functions by redirecting the activity of the CRL4DCAF15 ligase, leading to a reduction in RBM39 levels in WT KBM7 cells.

MGD-28 is a potent molecular glue degrader that demonstrates significant in vitro efficacy against various hematological cancer cell lines. It induces degradation of Ikaros family zinc finger proteins 1, 2, and 3 (IKZF1/2/3) and casein kinase 1 alpha (CK1α) with nanomolar potency via a Cullin-cereblon (CRBN) dependent pathway. Compared to lenalidomide and pomalidomide, MGD-28 achieves deeper, faster, and more potent degradation of these neosubstrates. Additionally, MGD-28 exhibits broad antiproliferative activity in multiple solid malignancies and shows preferential cytotoxicity toward multiple myeloma patient-derived cells at various disease stages.

dWIZ-1 is a first-in-class molecular glue degrader that specifically targets the WIZ transcription factor for proteasomal degradation, leading to potent induction of fetal hemoglobin (HbF) in erythroblasts. This novel compound functions by enhancing the interaction between CRBN and WIZ, demonstrating an EC50 of 547 nM for CRBN-WIZ complex formation.

dCeMM3 (Compound 3) is a molecular glue degrader that facilitates the ubiquitination and degradation of cyclin K. It achieves this by promoting an interaction between the CDK12-cyclin K complex and the CRL4B ligase complex.

MG-277, a molecular glue degrader, efficiently induces the degradation of the translation termination factor GSPT1, based on the Cereblon E3 ligand, with a DC50 of 1.3 nM. It potently inhibits tumor cell growth in a p53-independent manner, demonstrating IC50 values of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells. MG-277 exhibits significant anticancer activity.

SJ3149 is a highly selective and potent molecular glue degrader targeting CK1α protein, exhibiting broad antiproliferative activity. It is a valuable tool for cancer research.

dCeMM4 (Compound 5) is a molecular glue degrader that facilitates the ubiquitination and degradation of cyclin K. It achieves this by promoting an interaction between the CDK12-cyclin K complex and the CRL4B ligase complex.

dWIZ-2 is a molecular glue degrader of the WIZ transcription factor that robustly induce HbF in erythroblasts. dWIZ-2 shows improved pharmacokinetic (PK) properties than dWIZ-1.

MRT-6160 represents a groundbreaking molecular glue degrader designed to selectively target VAV1, achieving its proteasomal degradation with a DC50 value of 7 nM. This innovative compound showcases its unique mechanism and therapeutic potential.

DS17 is a high-efficiency molecular glue degrader that specifically induces the degradation of cyclin K, demonstrating remarkable potency with an EC50 of 13 nM. By exploiting the ubiquitin-proteasome system, DS17 effectively eliminates cyclin K, a critical regulator of transcription and cell cycle progression, positioning it as a valuable tool in cancer research and drug discovery.

ALV1 is a molecular glue degrader targeting Ikaros (IKZF1) and Helios (IKZF2), with DC50 values of 2.5 nM and 10.3 nM, respectively. It binds to CRBN with an IC50 of 0.55 µM and induces CRBN-Helios dimerization. ALV1 is a valuable tool for studying the properties and functions of regulatory T cells (Treg cells).

ZZ3 is a potent CDK12/13 molecular glue degrader with DC50 of 35 nM and 57 nM, respectively.

6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer.

HYNIC-FAPI-04 is a useful ligand for making [99mTc]Tc-HYNIC-FAPI-04. In vitro experiments, the results indicated that [99mTc]Tc-HYNIC-FAPI-04 showed binding properties, and inhibited the migration of tumor cells. The [99mTc]Tc-HYNIC-FAPI will be a promising SPECT/CT imaging probe.

NOP-1A standard. 11C-NOP-1A is a new radioligand for thenociceptin/orphanin FQ peptide (NOP) receptor, with high affinity (Ki, 0.15 nM) and appropriate lipophilicity (measured logD, 3.4) for PET brain imaging. 11C-NOP-1A is the the first successful radioligand to image NOP receptors in rat and monkey brain. 11C-NOP-1A is a selective antagonist at the NOP receptor and has high affinity and appropriate lipophilicity for blood–brain barrier permeability. 11C-NOP-1A imaging in rhesus monkeys showed high brain uptake and a large receptor-specific signal and could be quantified with the gold standard method of compartmental modeling. In humans 1C-NOP-1A reliably quantified NOP receptors in human brain both in large brain regions and at a voxelwise level using parametric imaging. The radiation absorbed dose in humans was similar to that observed with other 11C-labeled ligands and would allow multiple scans of a single subject. Thus, 11C-NOP-1A is a promising radioligand for reliably quantifying NOP receptors in human brain.

The Precursor of NOP-1A.  (11)C-NOP-1A is a useful radioligand for quantifying NOP receptors in the monkey brain, and its radiation dose is similar to that of other (11)C-labeled ligands for neuroreceptors.

HL-43 (EP4 antagonist HL-43) is a selective prostaglandin E receptor 4 (EP4) antagonist, promotes chondrocyte differentiation/cartilage regeneration and anabolism with low toxicity; HL-43 exhibits the highest potency in inducing Col2a1 expression and reducing Mmp3 expression in presence of IL-1β. HL-43 downregulats Mmp3/13 expression in a dose-dependent manner. HL-43 induces anabolic factors (ACAN and SOX9), and suppresses catabolic factor (MMP13), and hypertrophic marker (COLX), inhibits the STAT3 catabolic pathway;. HL-43 promotes chondrocyte differentiation and ECM generation, and inhibits matrix degradation in both human and mouse articular cartilage explants. HL-43 enhances cartilage repair and regeneration in different artilage defect (CD) animal models.