HSP90i-COCH2CH2-PEG4-NHBoc is a conjugate of the HSP90 Ligand and the linker. HSP90i-COCH2CH2-PEG4-NHBoc can be used for synthesis of LYTACs, such as dPDL1-4

dPDL1-4 is a potent and selective eHSPTAC eHSP90 PD-L1 degrader with DC50s of 7.77 μM and 6.52 μM in HeLa and B16F10 cells. dPDL1-4 bridges eHSP90 with the target protein, inducing lysosomal degradation. dPDL1-4 can degrade PD-L1 significantly and inhibits tumor growth. dPDL1-4 can be used for the study of cervical cancer and melanoma.

DDO3602 is a PARP1 HEMTAC degradation agent mediated by HSP90. DDO3602 has good anti-tumor activity and tumor selectivity. DDO3602 induces G2/M phase arrest, DNA damage, and inhibits cell migration by degrading PARP1 in MCF-7 cells (IC50 = 187 nM). DDO3602 can be used for research on cancer such as breast cancer.

AU-1421 is a potassium ion (K⁺) site-directed regulator that specifically acts on various cation transport ATPases. AU-1421 can distinguish between two different K⁺-sensitive phosphorylation intermediate (E2P) states: for non-K⁺ transport type ATPases (such as the sarcoplasmic reticulum Ca²⁺-ATPase), after binding to AU-1421, it mimics the agonistic effect of K⁺, significantly accelerating the hydrolysis (dephosphorylation) of E2P. For K⁺ transport type ATPases (such as the gastric mucosa H⁺/K⁺-ATPase and the renal Na⁺/K⁺-ATPase), after binding to AU-1421, it inhibits the hydrolysis of E2P, stabilizing the phosphorylated intermediate, thereby blocking the ion transport cycle. AU-1421 can be used to study the mechanism of the potassium ion pump.

Ligritinib (AB801) is an orally active AXL receptor tyrosine kinase inhibitor. Ligritinib blocks the downstream signaling pathway by inhibiting the kinase activity of AXL. Ligritinib can be used in cancer research, especially in combination with chemotherapy for non-small cell lung cancer (NSCLC).

(±)-Spiro-oxanthromicin A (Compound 4), a polyketide, is a K-Ras inhibitor with an IC50 of 26.7  μM. (±)-Spiro-oxanthromicin A can be isolated from soil-derived Streptomyces sp. (±)-Spiro-oxanthromicin A can mislocalize oncogenic mutant K-Ras from the plasma membrane of intact MDCK cells. (±)-Spiro-oxanthromicin A can be used for cancers research.

HPK1 ligand 3-dimethylph tetrahydropyridine is a Target Protein Ligand-Linker Conjugate. HPK1 ligand 3-dimethylph tetrahydropyridine can be used to synthesize PROTAC HPK1 Degrader-4.

BT-33 is a fuorinated macrobicyclic oxepanoprolinamide antibiotic with broad-spectrum activity against multidrug-resistant bacterial pathogens.

UC-38 (NSC-629243) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with anti-HIV activity.

AY 31906 is an orally active pyrimidine sulfonamide diuretic. AY 31906 exhibits potent diuretic and natriuretic activities in rats and dogs, along with relatively potassium-sparing properties. AY 31906 exhibits superior activity to Furosemide. AY-31906 also has antihypertensive effects and can be used in the research of cardiovascular diseases.

(S)-Ebalzotan is the S-form of Ebalzotan. Ebalzotan is a 5-HT1A receptor agonist with activity in the study of depression. Ebalzotan can serve as a precursor to important active pharmaceutical ingredients. The synthesis of Ebalzotan involves a multi-enzyme catalyzed reduction reaction to obtain saturated primary or secondary alcohols in high yields and high enantioselectivity.

S-cEt-U phosphoramidite is a modified phosphoramidite monomer that can be used for the oligonucleotide synthesis.

Morpholino G phosphoramidite (Compound 4b) is a nucleoside building block that is used for synthesis of morpholino oligonucleotides. Morpholino G phosphoramidite can be used for oligonucleotide therapies research.

Morpholino C phosphoramidite (Compound 4c) is a nucleoside building block that can be used for synthesis of morpholino oligonucleotides. Morpholino C phosphoramidite can be used for oligonucleotide therapies research.

5'-O-DMTr-Nap-dU-3'-CE Phosphoramidite is a phosphoramidite monomer used in nucleic acid synthesis, such as oligonucleotides.

DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite (Compound 5) is an RNAi agent and an inhibitor of Ataxin-2 (ATXN2). DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite can be studied in research on ATXN2-associated neurological diseases.

5'(E)-VP-2'-OMe-Bz-C Phosphoramidite is a phosphoramidite monomer used in nucleic acid synthesis, such as oligonucleotides.

Amb929 (ZINC000002782982), a nsp3 ligand, is an anti-SARS-CoV-2 agent. Amb929 inhibits SARS-CoV2-mNG replication in VeroE6 cells with an EC50 of 34.7 µM. Amb929 has limited and moderate cytotoxicity for VeroE6 cells (CC50: 281 µM). Amb929 also inhibits SARS-CoV-2-mNG replication in Human Airway Epithelium (HAE).

PD 175069 is a potent and selective N-type calcium channel antagonist with an IC50 of 0.32 μM. PD 175069 is efficacious in an audiogenic seizure model using DBA/2 mice. PD 175069 can be used for on neurological conditions such as neuropathic pain and stroke.

Patrinoside aglucone (Compound 8) is an iridoid glucoside that can be isolated from the Valeriana tuberosa. Patrinoside aglucone has potent anticancer activity with G2/M phase tumor cell cycle arrest and apoptosis induction. Patrinoside aglucone also significantly inhibits the proliferation of cancer stem cells (such as MDA-MB-231 and U-251MG cells). Patrinoside aglucone has great anti-inflammatory activity by inhibiting NO release (IC50: 43.44 μM) and significantly reduces the level of TNF-α, IL-1β, IL-6, PGE2 and COX-2.

Indazole 1 is a potent CDC2-like kinase 2 (CLK2) inhibitor (IC50=12.3 nM). Indazole 1 inhibits the phosphorylation of SR proteins (e.g., SRSF1, SRSF3) and modulates alternative splicing of Wnt signaling-related genes. Indazole 1 is promising for research of osteoarthritis.

NPC-15669 is a novel Mac-1 inhibitor. NPC-15669 reduces plasma levels of ET-1, TxB, prostacyclin, AT-III, and total protein S. NPC-15669 can be used in the research of myocardial infarction.

JY-5 is an E3 ligase ligand. JY-5 can be used for synthesis of PROTAC JY-21.

MSK-9 is a positive allosteric modulator of the P2X4 receptor with dual activities of enhancing ion conductance and delaying receptor inactivation. MSK-9 stabilizes the open state of the P2X4 receptor through rigid 3-piperidinyl and hydrophobic menthyl substituents. MSK-9 can be used in the study of multiple sclerosis (MS).

TIR-199 is a novel and highly specific dual proteasome inhibitor that can effectively inhibit the PSMB5 subunit of constitutive proteasome and the PSMB8 subunit of immunoproteasome. TIR-199 can induce the death of various tumor cells. TIR-199 can be used for research on myeloma.

GW 796406 is a novel vascular peptidase inhibitor. GW 796406’s inhibitory activity against NEP (IC50 ≈ 1.1-2.5 nM) is about three times that of ACE (IC50 ≈ 1.6-4.7 nM). GW 796406 can be used for research on cardiovascular conditions.

L-738872 is an orally active HIV-l encoded protease inhibitor. L-738872 inhibits the spread of HIV-1 in infected cells.

BE-16627B is a metalloproteinase inhibitor. BE-16627B can be isolated from microbial cultures. BE-16627B can inhibit metalloproteinases in enzyme assays. BE-16627B reduces the number and size of HT1080 cell nodules on lung surface in mouse models. BE-16627B inhibits growth of HT1080 cells in mice. BE-16627B can be studied in anti-cancer research.

K-Ras ligand-Linker Conjugate 8 is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for KRAS and a PROTAC linker, which recruits E3 ligases. K-Ras ligand-Linker Conjugate 8 can be used for synthesis of PROTAC KRAS(on) degrader ACBI-4.

(R)-MDL-101146 is the R-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis.