QR-6401 is a highly potent and selective macrocyclic CDK2 inhibitor with IV50 of 0.37 nM. QR-6401 exhibits good selectivity against other closely related kinases, such as CDK1, CDK4, CDK6, CDK9 and GSK3β. QR-6401 demonstrates robust antitumor efficacy in an OVCAR3 ovarian cancer xenograft model via oral administration.

JNJ-74856665 is an orally bioavailable, potent, and selective DHODH inhibitor with IC50 of 0.40 nM. JNJ-74856665 shows favorable physicochemical properties and has been selected for clinical development in patients with AML and myelodysplastic syndromes (MDS).

Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX1R and OX2R currently under clinical investigation as a novel therapy for insomnia.Suvorexant is an analytical reference standard categorized as a diazepane sedative.Formulations containing suvorexant show abuse potential similar to zolpidem in recreational polydrug users with a history of sedative and psychedelic drug use.2 Suvorexant is regulated as a Schedule IV compound in the United States. This product is intended for use in analytical forensic applications.

Sterculic acid is a stearoyl-CoA desaturase-1 (SCD1) inhibitor. Sterculic acid specifically inhibits the delta-9 desaturase (Δ9D) activity with an IC50 value of 0.9 μM.

DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [14C]

DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.

TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2, and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs.

Specific inhibitor of vaccinia-related kinase 1 (VRK1)-mediated phosphorylation of barrier-to-autointegration factor (BAF)

BPA-B9 (Bipyridine amide B9) is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=39 nM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells.

Orlistat is a drug designed to treat obesity. Orlistat's primary function is preventing the absorption of fats from the human diet by acting as a lipase inhibitor, thereby reducing caloric intake. Orlistat is intended for use in conjunction with a healthcare provider-supervised reduced-calorie diet.

A-61603 is a selective α1A-adrenergic receptor agonist. A-61603 increases the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro.

RGT-419B is a CDK inhibitor and not only actively inhibits CDK2, CDK4 and CDK6, but also demonstrates strong anti-proliferation activities.

RGT-587 is a CDK inhibitor and selectively inhibits CDK4 but also has excellent brain penetration.

ZZ2 is a YPEL5-GID/CTLH-dependent BRD4 degrader with CD50 of 169 nM.

ZZ1 is a YPEL5-GID/CTLH-dependent BRD4 degrader with CD50 of 502 nM. ZZ1 induces selective degradation of BET proteins (BRD3 and BRD4).

Z6466608628 is a CRBN molecular gluewith EC50 of 0.34 µM. Z6466608628 selectively recruits PPIL4, along with its binding partner DHX40.

Compound 23 (LRRK2 inhibitor) is a potent, selective, and CNS penetrant LRRK2 inhibitor with IC50 of 5 nM.

AK-1690 is the first, potent and selective PROTAC STAT6 degrader with DC50 of 1 nM. AK-1690 displays excellent microsomal and plasma stability, making it a suitable tool compound for in vivo studies.

BAY-405 is a potent and selective MAP4K1 inhibitor with IC50 of 6 nM. BAY-405 potentiates in vitro and in vivo antitumor T-cell reactivity which overcomes the suppression by TGFβ and PGE2.

Epitalon acetate is a synthetic tetrapeptide with anti-aging properties. Epitalon acetate reduces levels of lipid peroxidation products, delays age-related estrous shutdown, and decreases the frequency of bone marrow cell chromosomal aberrations in female mice. It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice. Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm.

A novel, second-generation C-terminal Hsp90 inhibitor with Kd of 191 and 726 uM for Hsp90α and Hsp90β, respectively.

Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC).

OSSL_325096 is a novel potent small mlolecule p97/VCP inhibitor, suppresses cell proliferation and induces ER stress and apoptotic cell death in MM cell lines (IC50=0.1-0.5 uM).

MTX-531 is a potent and selective inhibitor of EGFR and PI3K with IC50 of 15 nM and 6.4 nM, respectively. MTX-531 represents a unique single-molecule approach to balanced combination therapy that minimizes off-target effects while eliminating the need to optimize the pharmacokinetic profiles of multiple agents.

SX-682 (SX682) is a potent, allosteric, orally bioavailable inhibitor of CXCR1 and CXCR2.SX-682 enhances tumor infiltration, activation, and the therapeutic efficacy of adoptively transferred NK cells.SX-682 significantly inhibits trafficking of PMN-MDSCs without altering CXCR2 ligand expression.SX-682 enhances T cell-based immunotherapeutic efficacy.

TP-1454 is an activator of PKM2 with AC50 of 10 Nm in biochemical assays.TP-1454 modulates tumor-immune responses by destabilizing T-regulatory cells.

Novel Enrichable and MS-Cleavable Cross-linker to Define Protein-Protein Interactions by Mass Spectrometry

OTUB1/USP8-IN-1 is a potent dual OTUB1/USP8 inhibitor with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively. OTUB1/USP8-IN-1 can be used in research of cancer.

Snail/HDAC-IN-1 is a potent Snail/HDAC dual target inhibitor. Snail/HDAC-IN-1 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis.