RDR 02308 is a TLR4-MyD88 binding inhibitor that inhibits full-length β-lactamase.

FM04 is a potent P-glycoprotein (P-gp) inhibitor (EC50=83 nM). FM04 inhibits P-gp in 2 mechanism: (1)FM04 binds to Q1193, followed by interacting with the functionally critical residues H1195 and T1226; or (2)FM04 binds to I1115 (a functionally critical residue itself), disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling ICL2-NBD2 interaction and thereby inhibiting P-gp.

Thiotraniliprole (HY366) is an ortho formamidobenzamide insecticide that can be used for the synthesis of insecticidal combinations. Thiotraniliprole has potential applications in the prevention of lepidoptera pests, coleoptera pests, ants, and termites.

Didocosahexaenoin, an omega-3 derivative, is a diglyceride of DHA and can be synthesised from DHA triglycerides. Didocosahexaenoin causes significant loss of mitochondrial membrane potential and induces ROS production. Didocosahexaenoin induces apoptosis. Didocosahexaenoin induces stronger cytotoxicity than DHA in human prostate carcinoma cells.

PF-07059013 is an orally active and potent noncovalent modulator of sickled hemoglobin (HbS). PF-07059013 specifically binds to Hb with nanomolar affinity and displays strong partitioning into red blood cells (RBCs). PF-07059013 can be used for sickle cell disease (SCD) research.

JZ128 is a potential, irreversible, selective inhibitor of PKN3 with IC50  of 120 nM and shows a narrow kinome inhibition spectrum. JZ128 is used as a tool compound to identify novel potential PKN3 substrates.

BAY-297 is a potent and selective PIP4K2A inhibitor. BAY-297 can serve as valuable chemical probes to study PIP4K2A signaling and its involvement in pathophysiological conditions such as cancer.

IACS-15414 (IACS 15414) is a potent, selective, orally bioavailable SHP2 inhibitor with IC50 of 122 nM; IACS-15414 potently suppressed the mitogen-activated protein kinase (MAPK) pathway signaling and tumor growth in RTK-activated and KRASmut xenograft models in vivo. IACS-15414 potently suppressed the mitogen-activated protein kinase (MAPK) pathway signaling and tumor growth. IACS-15414 had excellent PK properties across species but a narrow hERG window.

BPR1R024 is an orally active and selective CSF1R inhibitor with IC50 of 0.53 nM. BPR1R024 specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth.

BMS-963272 is a potent, selective MGAT2 inhibitor with IC50 of 7.1 nM/18 nM (hMGAT2/mMGAT2) and shows excellent efficacy, safety, and tolerability profile.

JNJ-67569762 is a tetrahydropyridine-based BACE1 inhibitor targeting the S3 pocket with IC50 of 2.7 nM and shows 71-fold selectivity over BACE2.

GSK-3685032(GSK 3685032) is a first-in-class, potent, non-nucleoside, reversible, selective inhibitor of DNMT1 with IC50 of 0.036 μM. GSK3685032 induces robust loss of DNA methylation, transcriptional activation and cancer cell growth inhibition in vitro.

FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease.

AS-1763 is an orally available, potent, and selective BTK inhibitor and shows excellent potency against both wild/C481S mutant BTKs with IC50 of 0.85 nM/0.99 nM.

PZ703b is highly potent in killing BCL-XL dependent, BCL-2 dependent, and BCL-XL/BCL-2 dual-dependent cells in an E3 ligase (VHL)-dependent fashion.

UNC7145 is a negative control for UNC6934 (GLXC-22088).

(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models.

MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 53 nM and a log D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research.

BAY 1251152 (VIP152 ) is the first potent, selective, orally available PTEFb/CDK9 inhibitor with biochemical IC50 of 9 nM and MOLM13 cell IC50 of 29 nM, displays> 50-fold selectivity against other CDKs.

EEDi-5273 is an exceptionally potent and orally efficacious embryonic ectoderm development (EED) inhibitor with IC50 of 0.2 nM and inhibits the KARPAS422 cell growth with IC50 of 1.2 nM. EEDi-5273 demonstrates an excellent PK and ADME profile, and its oral administration leads to complete and persistent tumor regression in the KARPAS422 xenograft model with no signs of toxicity.

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression.

IACS-9779 is a Potent IDO1 Inhibitor Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme. IACS-9779 with a predicted human efficacious once daily dose below 1 mg/kg to sustain >90% inhibition of IDO1 displayed an acceptable safety margin in rodent toxicology and dog cardiovascular studies to support advancement into preclinical safety evaluation for human development.

VPC-70063 is a Myc-Max inhibitor. VPC-70067 is a close analog of the previously identified Myc inhibitor 10058-F4. VPC-70063, of a chemically different scaffold, was the best performer in a panel of in vitro assays, and the forerunner for future hit-to-lead optimization efforts.

A synthetic curcuminoid that selectively inhibits STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs.

MMPP is a novel potent inhibitor of pro-inflammatory responses by inhibiting in vitro STAT3 activation and its downstream signalling in murine macrophages and human synoviocytes from patients with RA.

LC28 is a novel inhibitor of STAT3 signaling, suppressing survival of cisplatin-resistant ovarian cancer cells.

SKLB-C2807 is an AR-DBD binder.

GSK743 is a Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitor.

GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media.