LD4172 is a highly potent and specific RIPK1 degrader with Ki of 4.8 nM. LD4172 enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy in female C57BL/6J mice.

ATX968 is a potent and selective inhibitor of DHX9 with IC50 of 8 nM and Kd of 1.3 nM, respectively. ATX968 induces robust and durable responses in an MSI-H/dMMR xenograft model but not in a microsatellite stable (MSS)/proficient mismatch repair (pMMR) model.

PRLX 93936 is a structural analogue of erastin with potential antineoplastic activity. Erastin analogue PRLX 93936 appears to inhibit mitochondrial outer membrane protein VDACs (voltage-dependent anion channels) 2 and 3, resulting in an oxidative, non-apoptotic cell death. Erastin analogue PRLX 93936 exhibits greater lethality in cell lines harboring mutations in the GTPase protein oncogenes HRAS and KRAS or the serine-threonine protein kinase oncogene BRAF than in non-tumorigenic cell lines. VDACs 2 and 3 are up-regulated in a wide variety of tumor cell lines.

OAT-177 is a potent, selective, orally active acidic mammalian chitinase (AMCase) inhibitor with IC50 of 14 and 19 nM against human and mouse AMCas, respectively, >150-fold selectivity over mCHIT1.

VU 0606170 (also referred to as VU0606170) is a selective inhibitor of the sodium-activated potassium channel KNa1.1, also known as Slack or Slo2.2. This compound has shown specificity for Slack channels over other related potassium channels, making it a valuable tool for studying the physiological and pathological roles of KNa1.1.

MG-002 is a second-generation, orally bioavailable inhibitor of eIF4A, a key RNA helicase involved in the initiation of cap-dependent mRNA translation. By targeting eIF4A, MG-002 effectively disrupts the translation of certain mRNAs, particularly those with complex 5' untranslated regions (UTRs) that are highly dependent on eIF4A activity. This mechanism of action makes MG-002 a promising candidate for targeting cancers and other diseases driven by dysregulated translation.

Novel potent broad-spectrum metallo-β-lactamase (MβL) inhibitor, inhibiting the MβLs NDM-1, VIM-2, ImiS, and L1

Novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupting Warburg metabolism and inducing context-dependent cytostasis in cancer cells

AM-5308 is a potent and selective KIF18A inhibitor with demonstrated antitumor activity in cell-based and animal models. Its ability to disrupt mitosis and induce cancer cell death makes it a promising candidate for further development as a cancer therapeutic.

Afoxolaner is an isoxazoline that inhibits insect and acarine ligand-gated chloride channels, in particular those gated by the neurotransmitter gamma-aminobutyric acid (GABA), blocking pre and post synaptic transfer of chloride ions across cell membranes.

HAPC-Chol is a cationic cholesterol. HAPC-Chol, as part of a lipoplex with DOPE, has been used for siRNA delivery and gene silencing in MCF-7 cells in a luciferase assay without affecting cell viability. It has also been used to deliver siRNA into mice via intravenous injection, resulting in HAPC-chol accumulation in the lungs.

Amoxicillin, also spelled amoxycillin and amox, is an antibiotic useful for the treatment of a number of bacterial infections. Amoxicillin is a broad-spectrum semisynthetic antibiotic similar to Ampicillin except that its resistance to gastric acid permits higher serum levels with oral administration. It is the first line treatment for middle ear infections. It may also be used for strep throat, pneumonia, skin infections, and urinary tract infections among others. It is taken orally. This drug acts by inhibiting the synthesis of bacterial cell walls. It inhibits cross-linkage between the linear peptidoglycan polymer chains that make up a major component of the cell walls of both Gram-positive and Gram-negative bacteria. It has two ionizable groups in the physiological range (the amino group in alpha-position to the amide carbonyl group and the carboxyl group).

AC-265347 is a calcimimetic acting agent and highly efficacious, orally active allosteric agonist (PAM) of CaSR with IC50 of 10 nM in PI hydrolysis assays.

Remlarsen (MRG-201), a miR-29b mimic, acts a miR-29b agonist. Remlarsen has the potential for preventiong formation of a fibrotic scar or cutaneous fibrosis.

CHIR-99021 HCl is a potent and selective inhibitor of glycogen synthase kinase 3 beta (GSK-3β), a key enzyme involved in regulating various cellular processes, including metabolism, cell proliferation, and differentiation. By inhibiting GSK-3β, CHIR-99021 HCl modulates downstream signaling pathways, particularly the Wnt/β-catenin pathway, leading to significant biological effects both in vitro and in vivo.

Laduviglusib (CHIR-99021) trihydrochloride is a well-characterized small molecule inhibitor that specifically targets glycogen synthase kinase-3 alpha and beta (GSK-3α/β). It exhibits potent inhibitory activity with IC50 values of 10 nM for GSK-3α and 6.7 nM for GSK-3β. Importantly, it demonstrates high selectivity, being over 500-fold more selective for GSK-3 compared to other kinases such as CDC2 and ERK2, as well as a broad range of other protein kinases.

VU0364739 is a selective inhibitor of phospholipase D2 (PLD2) with an IC50 value of 22 nM. Phospholipase D (PLD) enzymes, including PLD1 and PLD2, are involved in various cellular processes, such as signal transduction, membrane trafficking, and cytoskeletal reorganization. PLD2, in particular, has been implicated in cancer cell proliferation, survival, and metastasis, making it a potential target for anticancer therapies.

VU0364739 is a selective PLD2 inhibitor (IC50: 22 nM). VU0364739 decreases cancer cell proliferation.

H-Ile-Pro-Pro-OH, a milk-derived peptide, inhibits angiotensin-converting enzyme (ACE) with an IC50 of 5 μM. Antihypertensive tripeptides.

H-Ile-Pro-Pro-OH hydrochloride, a milk-derived peptide, inhibits angiotensin-converting enzyme (ACE) with an IC50 of 5 μM. Antihypertensive tripeptides.

EP055 (EP-055) is a small molecule that targets EPPIN on the surface of sperm and inhibits motility (IC50=199.5 uM, CASA assay using human sperm), binds to the C-terminal domain of EPPIN.

Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) consists the ADCs linker (Acetylene-linker-Val-Cit-PABC) and potent tubulin (MMAE). Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) is a drug-linker conjugate for ADC.

Ac-Lys-Val-Cit-PABC-MMAE is a drug-linker conjugate for ADC. Ac-Lys-Val-Cit-PABC-MMAE contains the ADC linker (peptide Ac-Lys-Val-Cit-PABC) and a potent tubulin polymerization inhibitor MMAE.

Bi-Mc-VC-PAB-MMAE consists ADCs linker (Fmoc-Val-Cit-PAB) and potent tubulin inhibitor (MMAE). Bi-Mc-VC-PAB-MMAE is a drug-linker conjugate for ADC.

PSMA-Val-Cit-PAB-MMAE is a novel small-molecule PSMA-targeted conjugate based on the monomethyl auristatin E for the chemotherapy of prostate cancer.

MTX-3937 is a small-molecule inhibitor targeting Siglec-9 (Sialic acid-binding immunoglobulin-type lectin-9), a member of the Siglec family of immunomodulatory receptors. Siglec-9 is primarily expressed on immune cells, such as myeloid cells and natural killer (NK) cells, and plays a role in regulating immune responses by transmitting inhibitory signals through its intracellular immunoreceptor tyrosine-based inhibitory motifs (ITIMs).

TH7126 is an inactive control of TH6342. TH7126 does not disrupt SAMHD1 dimerization.

TH7127 is a SAMHD1 inhibitor with IC50 of 4.9 μM/4.5 μM/4.0 μM against dGTP/Cl-F-ara-ATP/ara-CTP, respectively.