ZSH-2208 is a synthetic analog of all-trans retinoic acid (ATRA) designed to overcome resistance and improve differentiation therapy in acute promyelocytic leukemia (APL) and other malignancies. In published studies, ZSH-2208 has shown superior anti-proliferative and pro-differentiation activity compared to ATRA in ATRA-resistant APL cell lines such as NB4-R2. For example, ZSH-2208 induced significant G1 phase arrest and granulocytic differentiation in NB4-R2 cells at concentrations around 1–10 µM, whereas ATRA was largely ineffective at equivalent doses. In mouse xenograft models, ZSH-2208 treatment led to marked tumor growth inhibition without the rapid metabolic degradation seen with ATRA. These data suggest that ZSH-2208 is a promising candidate for treating retinoic acid-resistant leukemias and potentially other cancers sensitive to retinoid signaling.

JC19 is a a cysteine-reactive small molecule degrader of SARS-CoV-2 nsp14 with DC50 of 8.7 uM in HEK293T cells.

H203 is a potent dual Mdm2/MdmX inhibitor with Ki of 2/11 nM, respectively; H203 significantly reduced cell viability in the cells overexpressing both Mdm2 and MdmX, and a significant and dose-dependent decrease in cell number in H203-treated cells lacking Mdm2 or MdmX. H203-mediated decrease in cell viability is strictly p53-dependent and H203 affects MdmX more specifically than nutlin-3a. H203 induced the expression of the p21 gene but not the p53 gene in treated cancer cells.

ICT12035 (AZ2158) is a potent, selective formylpeptide receptor-1 (FPR1) antagonist with IC50 of 30 nM in calcium mobilisation assays (100 nM fMLF).

Compound 4 (VHL-CDO1 glue degrader) is a molecular glue degrader for cysteine dioxygenase 1 (CDO1) by recruiting it into the Von Hippel-Lindau (VHL) E3 ligase complex and leading to its selective degradation.

Cyclin K degrader DS17 is a selective cyclin K molecular glue degrader with TR-FRET EC50 of 19 nM.

MYC degrader 1 TFA (compound A80.2HCl) is an orally available molecular glue degrader targeting MYC, exhibiting significant anti-tumor activity. It restores pRB1 protein function and re-establishes the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors.

KT-333 diammonium is a molecular glue degrader that selectively targets STAT3 for proteasomal degradation by bridging interactions between STAT3 and the VHL E3 ubiquitin ligase complex. Exhibiting high specificity for STAT3 degradation, this compound demonstrates potent antitumor efficacy. Its therapeutic potential is particularly relevant in hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).

Pomalidomide-d4 is a deuterium-labeled analog of pomalidomide, a third-generation immunomodulatory drug functioning as a molecular glue degrader. This compound selectively binds the cereblon E3 ubiquitin ligase complex, triggering targeted proteasomal degradation of Ikaros family transcription factors—a key mechanism underlying its therapeutic activity.

KT-333 ammonium (Compound A) is a targeted molecular glue degrader that induces STAT3 protein degradation via the ubiquitin-proteasome pathway. The compound facilitates this process by simultaneously engaging both STAT3 and the VHL E3 ubiquitin ligase, demonstrating remarkable degradation selectivity. With potent antitumor efficacy, KT-333 ammonium shows particular promise for investigating therapeutic interventions in hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).

Pomalidomide-d5 is a deuterium-stabilized isotopologue of pomalidomide, a third-generation immunomodulatory drug that functions as a molecular glue degrader. This compound mediates targeted protein degradation by recruiting the cereblon E3 ubiquitin ligase to promote ubiquitination and proteasomal elimination of Ikaros family transcription factors (IKZF1/3), a mechanism central to its therapeutic activity.

MYC degrader 1 (compound A80.2HCl) is an orally available molecular glue degrader targeting MYC, with significant anti-tumor activity. It restores pRB1 protein function and re-establishes the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors.

VNPP433-3β is a first-in-class molecular glue degrader that simultaneously targets ​androgen receptor (AR), its splice variants (AR-Vs), and Mnk1/2 kinases for proteasomal degradation. This multimodal agent demonstrates potent anti-proliferative activity in ​castration-resistant prostate cancer (CRPC) models, with ​GI50 values of 0.2–0.31 μM in LNCaP, C4-2B, and CWR22Rv1 cells. Its robust in vivo efficacy, evidenced by ​tumor growth inhibition in CWR22Rv1 xenografts, is supported by favorable pharmacokinetics in CD-1 mice.

IKZF-IN-1 (Compound I) is a molecular glue degrader that selectively targets IKZF1/2/3/4 (Ikaros zinc finger family proteins) for proteasomal degradation. This immunomodulatory compound holds therapeutic potential for investigating cancer and viral infection treatment strategies.

LC-04-045 is a leading NEK7 molecular glue degrader with DC50 of 7 nM and Dmax of 90 % in MOLT-4 cells. LC-04-045 displays high selectivity for NEK7 across the proteome.

QXG-6442 is a potent molecular glue degrader targeting CK1α, demonstrating high degradation efficiency (DC50 = 5.7 nM, Dmax = 90%). This compound significantly suppresses proliferation in the MOLM-14 leukemia cell line, highlighting its therapeutic potential.

MRT-2359 a potent, selective and orally bioavailable GSPT1-directed molecular glue degrader (MGD).

SW394703 is a novel DDB1-dependent molecular glue degrader for cyclin K, SW394703 is toxic to HCT116 cells (IC50=1.2 uM).

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.

PVTX-405 is a potent, effective, highly selective, and orally efficacious IKZF2 molecular glue degrader with DC50 of  0.7 nM. PVTX-405 in combination with anti-PD1 or anti-LAG3 significantly increases animal survival compared to anti-PD1 or anti-LAG3 alone.

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.