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.

AM12814 is a potent and partial CB1 and CB2 agonist with Ki values of 0.7 nM and 3.4 nM. AM12814 can inhibit cAMP accumulation and recruitse β-arrestin 2. AM12814 exhibits cannabimimetic effects. AM12814 can be used for the research of neurological disease, suah as catalepsy.

RSL3-NH2-Ala-Val-DBCO-PEG4-Maleimide is a drug-linker conjugate for ADC. RSL3-NH2-Ala-Val-DBCO-PEG4-Maleimide consists of a GPX4 inhibitor and ferroptosis inducer (RSL3-NH2) and a linker (H-Ala-Val-OH). RSL3-NH2-Ala-Val-DBCO-PEG4-Maleimide can be used for synthesis of ADCs.

PD-161182 is a non-peptide NK-3 antagonist. PD-161182 can be studied in NK-3-related central nervous system disturbances, pain, inflammation, pulmonary and skin diseases.

PFI-7-O-C4-piperazin is a E3 ligase ligand-linker conjugate that can be used for synthesis of PROTACs, such as NEP162. The E3 ligase ligand (PFI-7) of NEP162 is a highly selective antagonist of GID4 (KD = 0.22 μM). NEP162 is a BRD4 PROTAC degrader with anti-tumor activity[1].

NEP162 is a BRD4 PROTAC degrader with DC50s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc.

tri(GalNAc-PEG2)-PEG4-cyclo(Ac-DCAW-{Arg(3F-Ph)-PEG2}-LGELVWCT) (Cys2-Cys12) is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.

AZD3409 is a prenyl inhibitor that exhibits inhibitory activity against both farnesyl transferase and geranylgeranyl transferase I. AZD3409 inhibits the growth of breast cancer cells, with IC50s of 220 nM (MDA-MB-468), 180 nM (MDA-MB-361), and 290 nM (SK-Br-3). AZD3409 significantly reduces the activation level of AKT in breast cancer cell lines. AZD3409 induces G0/G1 phase arrest in MDA-MB-468 cells, causes G2/M phase arrest in MDA-MB-361 cells. AZD3409 can be used for the study of breast cancer.

FE101120 is a non-peptide agonist CCK2 receptor agonist. FE101120 can be used for the study of diabetes.

MC-Gly-Gly-Phe-OSu is an ADC linker. MC-Gly-Gly-Phe-OSu can be used for the research of cancer.

WP-1034 is a JAK-STAT inhibitor with proapoptotic and antileukemic activity in acute myeloid leukemia (AML). WP-1034 blocks activation of Stat 3 and 5. WP-1034 induces cell cycle arrest and triggers apoptosis. WP-1034 can be used for AML research.

SB 414240 is a selective neurokinin-2 receptor (NK-2R) antagonist with Kis of 1 nM and 193 nM for human NK-3R and human NK-2R, respectively. SB 414240 does not bind the human μ-opioid receptor (hMOR). SB 414240 can be used for the study of neurological disease.

Boc-4-(3-oxobutyl)piperidine-(S,R,S)-AHPC is an E3 ligase ligand-linker conjugatecan be used in the synthesis of PROTAC BRD2 BD1 Degrader-1.

SK2220691 is a potent TRPV4 inhibitor. SK2220691 inhibits pulmonary edema induced by GSK1016790. SK2220691 inhibits HCl-induced increases in key factors such as VEGF, keratinocyte-derived chemokine (KC; CXCL1), and granulocyte colony-stimulating factor (GCSF).