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IRAK4/FLT3 inhibitor
Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation. - Edratide (TV 4710) is a synthetic peptide of 19 amino acid based on the complementarity-determining region 1 (CDR1) of a human anti-DNA antibody that expresses a major idiotype denoted 16/6 Id. Edratide reduces the rates of apoptosis (Apoptosis) and down-regulates of caspase-8 and caspase-3, up-regulates Bcl-xL. Edratide has the potential for the research of systemic lupus erythematosus (SLE).
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mGluR II agonist
Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus. -
analgesic agent
Tetrahydropalmatine, an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats. -
Anticancer agent
Flavokawain A is found in Piper methysticum (kava plant). It suppresses expression of iNOS and COX-2 in macrophages, decreases expression of Ki67, XIAP and survivin in urothelial cell carcinoma cells, and inhibits degradation of NF-kB.
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HMGB1 release inhibitor
Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent. -
Alkaloid
Conophylline is a vinca alkaloid derived from the leaves of the tropical plant Ervatamia microphylla. This compound functions as a differentiation inducer for pancreatic cells and demonstrates potent biological activity by suppressing hepatic stellate cells (HSC) while inducing apoptosis. It is of particular interest in research focused on pancreatic differentiation and the modulation of liver fibrosis. -
Rac1/Cdc42 Inhibitor
AZA1 is a potent dual inhibitor of Rac1 and Cdc42, key regulators of cell signaling pathways. This compound has been shown to induce apoptosis in prostate cancer cells while simultaneously inhibiting their proliferation, migration, and invasion. AZA1 serves as a valuable tool for research into the molecular mechanisms of prostate cancer progression and potential therapeutic interventions. -
Tyrosinase Inhibitor
Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells. -
HDAC Inhibitor
HC-Toxin is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 30 nM. This cyclic tetrapeptide effectively induces apoptosis in tumor cells, demonstrating significant anticancer activity. Its mechanism of action makes it valuable for research in cancer therapy and the modulation of gene expression. -
Apoptosis Inducer
epi-Eriocalyxin A is a diterpenoid compound that serves as an apoptosis inducer in colon cancer cells. It effectively inhibits the activation of ERK1/2 and JNK pathways, leading to the suppression of Bcl-2 expression. This compound is valuable for research focused on cancer treatment and the mechanisms of apoptosis. -
Cdc42 GTPase Inhibitor
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines. -
Monounsaturated Fatty Acid
Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activator. -
Iron Chelator
Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19. -
Anticancer Agent
(+)-Erinacin A (Erinacine A) is a cyanoditerpenoid isolated from Hericium erinaceus with anticancer, anti-inflammatory and neuroprotective activities. (+)-Erinacin A can induce cancer cell death by activating extrinsic and intrinsic apoptosis pathways. (+)-Erinacin A can also inhibit the expression of NO synthase (iNOS) and the production of nitrotyrosine to exert inflammatory and neuroprotective effects, thereby reducing ischemic brain damage. -
Ionophore
Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines . -
Topoisomerase IV Inhibitor
Ciprofloxacin is a potent topoisomerase IV inhibitor that demonstrates significant antibacterial activity as a fluoroquinolone antibiotic. It induces both mitochondrial and nuclear DNA damage, leading to mitochondrial dysfunction and increased reactive oxygen species (ROS) production. Ciprofloxacin exhibits anti-proliferative properties and triggers apoptotic pathways, making it a valuable tool for research applications focused on bacterial infections, oxidative stress, and cancer biology. -
Tubulin Inhibitor
Demecolcine is a potent tubulin inhibitor that effectively disrupts microtubule polymerization, exhibiting an IC50 value of 2.4 μM. By binding to tubulin dimers, Demecolcine exerts anti-mitotic effects, hindering cellular division. This compound is primarily utilized in research related to inflammatory disorders and various cancer pathways, making it valuable for studies focused on cell cycle regulation and targeted therapies. -
AMPK Agonist
10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis. -
Cysteine Residues Modifier
N-Ethylmaleimide (NEM) is a potent chemical reagent that irreversibly alkylates free sulfhydryl groups, specifically targeting cysteine residues. This compound serves as an effective inhibitor of cysteine proteases and significantly affects phosphate transport in mitochondria. With an IC50 value of 6.3 μM, N-Ethylmaleimide is valuable for modifying cysteine residues in proteins and peptides, making it an essential tool in biochemical research and studies involving protein functionality and structure. -
Apoptosis Inducer
Sanguinarine chloride is a benzophenanthridine alkaloid that functions as an apoptosis inducer primarily through the generation of reactive oxygen species (ROS). This compound is known to activate key signaling pathways, specifically JNK and NF-κB, facilitating programmed cell death. Sanguinarine chloride is widely utilized in cancer research and studies investigating apoptotic mechanisms. -
α-mannosidase inhibitor
Swainsonine (also known as Tridolgosir) is a naturally occurring indolizidine alkaloid and a potent, reversible inhibitor of α-mannosidase. By interfering with glycoprotein processing, Swainsonine disrupts key cellular signaling pathways, leading to apoptosis and G₂/M phase cell cycle arrest. It exhibits significant antitumor activity and has been widely studied for its potential role in cancer therapeutics and glycosylation-related biological processes. -
ENL PROTAC Degrader
MS41 is a selective PROTAC degrader of eleven-nineteen leukemia (ENL), with DC₅₀ values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). MS41 effectively inhibits the proliferation of ENL-dependent leukemia cells, induces G1 phase cell cycle arrest, and promotes apoptosis. It reduces chromatin occupancy of the ENL-associated transcription elongation complex, thereby suppressing oncogenic gene expression and leukemia progression. -
CECR2 inhibitor
NVS-CECR2-1 is a potent and selective non-BET family bromodomain (BRD) inhibitor targeting cat eye syndrome chromosome region, candidate 2 (CECR2). It binds CECR2 BRD with high affinity (IC50 = 47 nM; KD = 80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis in various cancer cells through both CECR2-dependent and CECR2-independent mechanisms. -
Gαq/11/14 Inhibitor
FR900359 is a cyclic depsipeptide and a selective inhibitor of Gαq/11/14 proteins in mammals. By targeting Gαq signaling, it effectively inhibits downstream pathways such as the ERK cascade. FR900359 has demonstrated the ability to suppress melanoma cell proliferation, lower blood pressure, and protect against airway hyperreactivity in murine models of allergen sensitization, such as the ovalbumin-induced asthma model. -
LSD1 inhibitor
Bomedemstat (IMG-7289) is an orally active, irreversible inhibitor of lysine-specific demethylase 1 (LSD1). By inhibiting LSD1, it increases methylation of histone marks H3K4 and H3K9, leading to altered gene expression. Bomedemstat exhibits potent anti-cancer activity by inhibiting cancer cell proliferation and inducing apoptosis, and is being explored as a therapeutic agent in hematologic malignancies and other cancers. -
Menin-KMT2A inhibitor
Bleximenib (JNJ-75276617) is an orally active and highly selective menin–KMT2A (MLL) interaction inhibitor, with IC50 values of 0.1 nM in humans, 0.045 nM in mice, and ≤0.066 nM in dogs. It effectively inhibits the proliferation of tumor cells and induces apoptosis and differentiation, particularly in malignancies driven by KMT2A rearrangements. Bleximenib is a promising therapeutic candidate for the study and treatment of leukemia and other menin-dependent cancers. -
Menin-KMT2A inhibitor
Bleximenib (JNJ-75276617) oxalate is an orally active and highly selective inhibitor of the menin–KMT2A (MLL) interaction, with IC50 values of 0.1 nM in humans, 0.045 nM in mice, and ≤0.066 nM in dogs. It effectively inhibits tumor cell proliferation and induces apoptosis and differentiation, particularly in cancers driven by KMT2A rearrangements. Bleximenib oxalate is a promising candidate for research in leukemia and other menin–KMT2A-dependent malignancies. -
APE1/REF-1 redox inhibitor
APX2009 is a specific inhibitor of APE1/REF-1 redox activity with demonstrated anticancer properties. It reduces the proliferation, migration, and invasion of breast cancer cells and induces apoptosis. APX2009 holds potential for targeted cancer therapy by disrupting redox-regulated transcription factors involved in tumor progression. - L-Asparaginase (L-ASNase) is a deamidating enzyme that catalyses the hydrolysis of L-asparagine and L-glutamine, and can be used for the research of acute lymphoblastic leukemia. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis.
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DNA Alkylator
Illudin S is a natural sesquiterpene compound with potent cytotoxic, anti-tumor, and antiviral activities. It exhibits genotoxic effects and disrupts cell cycle progression by blocking the G1-S phase transition in human leukemia cells. Illudin S is of interest in cancer research due to its ability to target rapidly proliferating cells. -
Osteoclast formation inhibitor
ABD56 is a bioactive compound that inhibits osteoclast formation and induces osteoclast apoptosis. Its mechanism of action involves suppression of the NFκB and ERK signaling pathways, making it a promising candidate for research in bone metabolism and osteolytic diseases. -
PGAM1 inhibitor
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC). - 7-Hydroxyflavone is an orally active flavonoid isolated from *Clerodendrum phlomidis*, exhibiting notable anti-inflammatory activity. It protects renal cells from nicotine-induced cytotoxicity through activation of the ERK/Nrf2/HO-1 signaling pathway. Additionally, 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM, and suppresses COX-2 and 5-LOX with IC50 values of 27 μg/mL and 33 μg/mL, respectively.
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Endoplasmic Reticulum Stress Inhibitor
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects. -
TrkB activator
HIOC is a potent and selective activator of the TrkB (tropomyosin receptor kinase B) receptor, capable of crossing both the blood-brain and blood-retinal barriers. It activates the TrkB/ERK signaling pathway, reduces neuronal apoptosis, and has been shown to attenuate early brain injury following subarachnoid hemorrhage (SAH). Additionally, HIOC exhibits neuroprotective effects in animal models of light-induced retinal degeneration. -
Apoptosis activator
Sulforaphene, a natural compound isolated from radish seeds, exhibits an ED₅₀ of approximately 2 × 10⁻⁴ M against velvetleaf seedlings. It promotes apoptosis and inhibits migration in cancer cells by suppressing signaling pathways including EGFR, phosphorylated ERK1/2 (p-ERK1/2), and NF-κB. -
EGFR inhibitor
Avitinib (Abivertinib) maleate is a third-generation, irreversible, and orally active selective EGFR inhibitor with IC50 values of 0.18 nM for both EGFR^L858R and EGFR^T790M, and 7.68 nM for wild-type EGFR. In addition to its EGFR-targeting activity, Avitinib maleate also inhibits BTK phosphorylation and induces apoptosis in mantle cell lymphoma models, demonstrating broad-spectrum anticancer efficacy. -
Autophagy inducer
Cearoin is a bioactive compound that promotes both autophagy and apoptosis by inducing reactive oxygen species (ROS) production and activating the ERK signaling pathway. Through this dual mechanism, cearoin contributes to the regulation of cellular stress responses and programmed cell death. Its ability to modulate these processes makes it a valuable candidate for research in cancer biology and other diseases involving dysregulated autophagy or apoptosis. -
Anticholinergic agent
Penehyclidine hydrochloride (also known as Penequinine hydrochloride) is a selective anticholinergic agent that acts as an antagonist of muscarinic M1 and M3 receptors. It exerts anti-inflammatory effects by modulating immune signaling in lung tissue, notably through activation of the NF-κB pathway and inhibition of pro-inflammatory cytokine release. In preclinical studies, Penehyclidine hydrochloride has been shown to alleviate pulmonary inflammation in rat models of chronic obstructive pulmonary disease (COPD), particularly under conditions of mechanical ventilation. These properties suggest its potential utility in managing respiratory inflammatory conditions and improving outcomes in mechanically ventilated patients with COPD. -
CBSI inhibitor
MY-673 is a colchicine binding site inhibitor (CBSI) that disrupts microtubule dynamics by inhibiting tubulin polymerization. In addition to its antimitotic effects, MY-673 suppresses the ERK signaling pathway, which leads to modulation of SMAD4 protein expression within the TGF-β/SMAD signaling axis. These combined actions result in potent inhibition of cancer cell proliferation and migration, and the induction of apoptosis, both in vitro and in vivo. MY-673 holds promise as a therapeutic candidate for targeting cancers driven by aberrant microtubule dynamics and dysregulated TGF-β/ERK signaling. -
Endogenous Metabolite
Gamma-linolenic acid (γ-linolenic acid, GLA) is an orally active omega-6 unsaturated fatty acid with broad pharmacological activities. It exhibits anti-inflammatory effects by inhibiting the NF-κB signaling pathway and suppressing the phosphorylation of ERK1/2 and JNK, key mediators of inflammatory responses. GLA also induces apoptosis in cancer cells, contributing to its anticancer potential. Additionally, it possesses antioxidant properties and has been shown to improve memory function, suggesting neuroprotective benefits. These multifunctional effects position gamma-linolenic acid as a promising compound for research in inflammation, oncology, and neurological disorders.

