Rodin-C is a selective HDAC inhibitor with IC50s of 0.059, 0.18   and 5.39 μM for HDAC1, HDAC2 and HDAC11, respectively, over HDAC3-10. Rodin-C significantly inhibits the HDAC-CoREST complex with low hematological toxicity. Rodin-C can be used for neurologic disorders such as Alzheimer’s disease research.

Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.

NASA-linker-VH032-PEG3 ligand is a ligand that can be used to synthesize PROTACs.

N-Demethylonalespib is a ligand for E3 ligase. N-Demethylonalespib can be used for synthesis of DDO3602.

Thalidomide-N-C-piperidine-C7-Br, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and a linker. Thalidomide-N-C-piperidine-C7-Br can be used in the synthesis of ZS3-046.

SK2187 is a selective AURKA PROTAC degrader with a DC50 of about 10 nM. SK2187 exhibits growth inhibition against NGP cells with an IC50 of 101.5 nM. SK2187 can be used for the study of MYCN-amplified neuroblastoma.

Thalidomide-piperidine-azetidine-Br is an E3 ligase ligand-linker conjugate that incorporates the Thalidomide based CRBN ligand and linker. Thalidomide-piperidine-azetidine-Br can be used for synthesis of BY13.

DBCO-HS-PEG2-VA-PABC-SG3199 is a drug-linker conjugate for ADC. DBCO-HS-PEG2-VA-PABC-SG3199 consists of a SG3199) based DNA small channel crosslinker and cleavable linker. DBCO-HS-PEG2-VA-PABC-SG3199 can be used for synthesis of ADCs.

DBCO-PEG9-amine (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. DBCO-PEG9-amine (TFA) is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

BTK ligand 11-alcohol-PEG6-azido is a synthesized E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs, such as TDP-43 degrader-1.

CDD-2212 is a STK33 inhibitor, with a Kd of 1.9 nM and an IC50 of 999 nM. CDD-2212 has relatively weak inhibitory effects on off-target kinases, with IC50 values of 3223 nM for CLK1, 1555 nM for CLK2, 5884 nM for CLK4, and 1093 nM for RET. CDD-2212 can be used for the study of contraception.

Fumiporexant (Compound Example 93) is an orally active, brain-penetrant and selective Orexin receptor 2 (OX2R) antagonist. Fumiporexant regulates the sleep-wake cycle and emotion-related pathways in the central nervous system. Fumiporexant is promising for research of nervous system diseases such as insomnia and major depressive disorder.

ACP3 ligand 1 (compound I11a) is a ligand against Acid Phosphatase 3 (ACP3, ACPP). ACP3 ligand 1 interacts with ACP3 expressed on the surface of tumor cells for in vivo pharmaco-delivery applications.

CDD-2211 is a STK33 inhibitor, with a Kd of 0.018 nM and an IC50 of 5 nM. CDD-2211 has relatively weak inhibitory effects on off-target kinases, with IC50 values of 115 nM for CLK1, 48 nM for CLK2, 187 nM for CLK4, and 78 nM for RET. CDD-2211 can be used for the study of contraception.

GRL-098-22 (Compound 6t) is a potent inhibitor targeting G protein-coupled receptor kinase 5 (GRK5) and GRK6 with IC50 values of 0.6 μM and 0.19 μM, respectively. GRL-098-22 is promising for research of diseases such as heart failure and multiple myeloma.

QPyN16Th is an N-palmitoylated cationic thiazolidine antibiotic. QPyN16Th is selectively active against the Gram-positive bavteria E. faecalis, S. aureus and MRSA with an MIC of 1.95 μM over gram-negative bacteria. QPyN16Th can induce membrane permeabilization and depolarization and ROS production in MRSA. QPyN16Th increases the survival of zebrafish model of intramuscular MRSA infection.

Bay-02752 (Bay o 2752) is a lipid-lowering agent. Bay-02752 inhibits acyl-CoA activity in liver microsomes (IC50 = 0.95 μg/mL). Bay-02752 inhibits intestinal cholesterol absorption in rats. Bay-02752 inhibits gallstone formation in hamsters.

SUAM 1221 is a prolyl endopeptidase inhibitor. CS-0777 can be used in the research of Alzheimer diseases.

DBCO-PEG4-VA-PABC-MMAE is a drug-linker conjugate for ADC. DBCO-PEG4-VA-PABC-MMAE consists of a tubulin inhibitor (MMAE) and a cleavable linker (DBCO-PEG4-VA-PABC). DBCO-PEG4-VA-PABC-MMAE can be used for synthesis of ADC ABBV-400.

K-Ras ligand-Linker Conjugate 6 formate incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 formate can be used in the synthesis of PROTAC K-Ras Degrader-1), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.

NC-2100 is a PPAR activator. NC-2100 can effectively reduce the plasma glucose and triglyceride levels of obese KKAy mice. NC-2100 can induce UCP1 and UCP2 expression in mesenteric and subcutaneous WAT of mice. NC-2100 can be used in research related to type 2 diabetes.

Dihydrouracil-Ph-2-Me-piperidine is an E3 ligase ligand. Dihydrouracil-Ph-2-Me-piperidine can be used to synthesize PROTAC HPK1 Degrader-6.

Acetoxycycloheximide is an antibiotic with antitumor activity. Acetoxycycloheximide a protein synthesis inhibitor. Acetoxycycloheximide significantly induces activation of procaspase-3 and subsequent apoptosis mediated by the Cytochrome c from mitochondria via activation of JNK pathway. Acetoxycycloheximide triggers the downregulation of cell surface TNF-R1 via the activation of ERK and p38 MAPK, thereby preventing activation of the NF-κB signaling pathway by TNF-α. Acetoxycycloheximide is much more toxic to female rats than to males. Acetoxycycloheximide can be used for inflammatory and immune diseases and cancers research.

MGD-22, a molecular glue, is an orally active IKZF1/2/3 degrader with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. MGD-22 exhibits extremely potent anti-proliferative activity against diverse hematological cancer cells. MGD-22 induces apoptosis in cancer cells. MGD-22 demonstrates potent anti-tumor efficacy in mice bearing NCI-H929 xenografts or WSU-DLCL-2 xenografts. MGD-22 can be used for the study of hematological cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL).

JQ1-S(GlcNAc)Cq is a sugar-coated BRD4 PROTAC degrader. JQ1-S(GlcNAc)Cq can inhibit the formation of the ternary complex between CRBN and BRD4(BD1/BD2). JQ1-S(GlcNAc)Cq can be used for the research of cancer.

AGM-130 is a cyclin-dependent kinase (CDK) inhibitor. AGM-130 exhibits antitumor activity.

LP-661438 (Compound 10) is an orally active DCK inhibitor (IC50 = 1.7 nM). LP-661438 inhibits deoxycytidine kinase in T cells and in vivo.

GSK256471 is a non-peptide tachykinin NK3 receptor antagonist with a pKi of 8.9 for the human recombinant NK3 receptor and 8.4 for the guinea pig native receptor. GSK256471 exhibits >100-fold selectivity for NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 noncompetitively inhibits neurokinin B (NKB)-induced inositol phosphate accumulation, and this inhibition is irreversible. GSK256471 inhibits wet dog shaking behavior and suppresses dopamine release. GSK256471 could be used to study schizophrenia.

(S,R,S)-AHPC-Me-amide-C15-acid is a synthesized E3 ligase ligand-linker conjugate that can be used for synthesis of PROTACs such as C199.

C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity.