KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.

GSM III is a γ-Secretase complexe (GSEC) modulator. GSM III significantly regulates amyloid-β (Aβ) length at the extracellular interface between the protease (NCT, PSEN) and the substrate APPC99. GSM III can be used for Alzheimer's disease (AD) research.

3'2'-cGAMP (c[A(2',5')pG(3',5')p]) disodium is the disodium of 3'2'-cGAMP). 3'2'-cGAMP (c[A(2',5')pG(3',5')p]) is a cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) isomer. 3'2'-cGAMP exhibits high selectivity for Drosophila STING (dSTING), activating the dSTING-NF-κB signaling pathway, inducing the expression of Sting-regulated genes (Srg) and conferring a potent antiviral state in vivo. 3'2'-cGAMP is resistant to cleavage by viral poxins. 3'2'-cGAMP can be used for the study of viral infections.

3'2'-cGAMP (c[A(2',5')pG(3',5')p]) is a cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) isomer. 3'2'-cGAMP exhibits high selectivity for Drosophila STING (dSTING), activating the dSTING-NF-κB signaling pathway, inducing the expression of Sting-regulated genes (Srg) and conferring a potent antiviral state in vivo. 3'2'-cGAMP is resistant to cleavage by viral poxins. 3'2'-cGAMP can be used for the study of viral infections.

Lepetegravir (Example 24) is a HIV integrase inhibitor. Lepetegravir has antiviral effects (EC50: 0.98 nM in MT-4 cells).

DRF-4848 is a COX-2 inhibitor. DRF-4848 can be used for the research of inflammation.

CW8001 is a covalent XPO1 (Exportin-1) inhibitor with an EC50 value of 1 nM for inhibiting T cell activation. CW8001 prevents nuclear localization of NFAT transcription factors, suppressing expression of inflammatory cytokines like IL-2. CW8001 is promising for research of T cell-driven immune diseases such as graft-versus-host disease (GVHD).

AKI-001 is an inhibitor of aurora kinase with cellular potency of IC50 of less than 100 nM. AKI-001 shows low nanomolar potency against Aurora A and Aurora B enzymes.

RBN010860 (example 150) is a potent PARP7 inhibitor with an IC50 of <0.1 μM. RBN010860 can be used for the study of cancer.

Dalpiciclib (isethionate) is a CDK4/6 inhibitor. Dalpiciclib (isethionate) inhibits the kinase activity of CDK4 and CDK6, thereby blocking the G1-to-S phase transition of the cell cycle and suppressing abnormal cell proliferation. Dalpiciclib (isethionate) can be used for the study of breast cancer.

Mansonone E (Compound 5) is a pesticide. Mansonone E can be isolated from heartwood of Mansonia gagei. Mansonone E has significant antifungal activity against Cladosporium cucumerinum, Candida albicans and Phytophthora parasitica. Mansonone E has potent antibacterial activity with MIC50s of both 7.8 μg/mL for Xanthomonas oryzae pv. oryzae and X. oryzae pv. Oryzicola. Mansonone E also has antifeedant and herbicidal activities.

FKBP12 ligand-2 (compound d) is a high affinity ligand targeting FKBP12. FKBP12 ligand-2 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-2 can be used for selective cancer research based on differences in intracellular presenter protein levels.

Forvisirvat (SP-624) is an orally active, brain-penetrant and selective sirtuin 6 (SIRT6) activator. Forvisirvat activates the deacetylase activity of SIRT6, enhancing DNA repair and mitochondrial health, and exhibits antidepressant activity in animal models. Forvisirvat is promising for research of major depressive disorder.

NK-611 is an epipodophyllotoxin derivative. NK-611 induces DNA double-strand breaks by inhibiting topoisomerase II (IC50 = 56 μM). NK-611 does not inhibit microtubule polymerization, thus avoiding the side effects of the parent compound, Podofilox. NK-611 exhibits broad-spectrum antitumor activity and demonstrates potent efficacy in in vivo models of leukemia. NK-611 can be used in cancer research.

F-14512 hydrochloride is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 hydrochloride enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 hydrochloride exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 hydrochloride demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 hydrochloride could be used to study breast cancer.

GI-149893 is a selective topoisomerase I (TopoI) inhibitor. GI-149893 prevents DNA religation and induces irreversible DNA damage in tumor cells. GI-149893 is promising for research of cancers (e.g., colon carcinoma HT-29/SW-48, breast MX-1, prostate PC-3 xenografts).

HB-35018 is an antifungal agent. HB-35018 inhibits the activity of acetyl lactate synthase (ALS) by covalently binding to its Lys310 residue. HB-35018 has good security. HB-35018 can be used for research on fungal infections.

MT-110 (BPN-0027490) is a selective and blood-brain barrier permeable non-muscle myosin II inhibitor. MT-110 markedly improves tolerability by selectively targeting NMII over CMII. MT-110 can be used the study of neurological disease.

YM-1 (TFA) is an inhibitor of angiotensin converting enzyme (ACE) that can be obtained from Chrysanthemum boreale Makino.

SJL 01 (Compound 8) is an anti-parasitic agent. SJL 01 (Compound 8) is cytotoxic to L-6 myocytes and exhibits antileishmaniasis activity both in vivo and in vitro. SJL 01 can be used for visceral leishmaniasis research.

Oxide-DFHBI-demethyl-C6-NH2 is a Target Protein Ligand-Linker Conjugate that incorporates a target aptamer ligand and a PROTAC linker, which recruits E3 ligases. Oxide-DFHBI-demethyl-C6-NH2 can be used for synthesis of RNA aptamer-based PROTAC Dth

Chlorozotocin (NSC 178248) is a glucose-based chloroethylnitrosourea with low myelotoxicity for studying leukemia in mice.

(+)-Arhalofenate ((+)-MBX 102) is the less active enantiomer of Arhalofenate. Arhalofenate is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.

L-163017 is a potent, orally active and nonpeptide angiotensin II receptor (AT) antagonist. L-163017 can inhibit prevent the pressor response to angiotensin II and reduce blood pressure. L-163017 can be used for the research of cardiovascular disease, such as hypertension.

Ro 17-1812 is a benzodiazepine receptor partial agonist with anticonvulsant effect.

Fmoc-Val-Lys-PAB-Exatecan is a derivative of Exatecan (DX-8951). Fmoc-Val-Lys-PAB-Exatecan can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. Fmoc-Val-Lys-PAB-Exatecan is often combined with CD70 mAb to form ADC drugs for the study of tumors with high CD70 expression.

SB 204144 is an HIV protease inhibitor. SB 204144 can be used in research on immune system diseases.

GR 250495X is an inhaled glucocorticoid receptor agonist. GR 250495X is designed as a antedrug, which takes effect locally in the lungs but is rapidly metabolized and inactivated in the bloodstream after entering the systemic circulation, thereby minimizing systemic side effects. GR 250495X can be used in asthma research.

YM-534, an imidazole compound, is an anti-cancer agent. YM-534 inhibits HL-60 cells with an IC50 of 2.5 μM. YM-534 retards the processing of preribosomal to ribosomal RNA of HL-60 cells. YM-534 can be used for the study of promyelocytic leukemia.

CGP 43487 is a NMDA receptor antagonist. CGP 43487 significantly affects the gross structural characteristics of the developing dentate gyrus.