Apoptosi

DNMT-IN-4 (Compound 4d) is a DNMT inhibitor with an IC50 value of 5.78 µM. It induces apoptosis and exhibits anticancer activity.

PD-1/PD-L1-IN-9, with an IC50 of 3.8 nM, is a potent and orally active inhibitor of the PD-1/PD-L1 interaction.

Antitumor agent-198 (Compound A3) exhibits cytotoxicity in head and neck squamous cell carcinoma (HNSCC) cells, effectively inhibiting the proliferation of CAL27, HN6, HN30, SCC9, and SCC25, with an IC50 ranging from 4 nM to 77 nM. Additionally, Antitumor agent-198 suppresses HNSCC cell migration, arrests the cell cycle, and induces apoptosis.

Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.

CDK9-IN-36 (Compound T7) is a potent, selective, and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. It effectively suppresses the proliferation of Osimertinib-resistant NSCLC cells by downregulating Mcl-1, reducing colony formation, and inducing apoptosis. Additionally, CDK9-IN-36 exhibits antitumor activity in xenograft models.

Tubulin polymerization-IN-73 (Compound 37) is an inhibitor of microtubule polymerization with an IC50 of 1.8 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in A549 cells. The compound inhibits the proliferation of both A549 WT and A549/T resistant cells with IC50 values of 0.023 μM and 0.057 μM, respectively. Additionally, Tubulin polymerization-IN-73 demonstrates antitumor activity in mouse models.

10-SLF is a PROTAC FKBP12 degrader. It facilitates the formation of a ternary complex between FKBP12 and FBXW7-R465C, leading to the proteasomal degradation of FKBP12 in a FBXW7-R465C-dependent manner. 10-SLF selectively reduces FKBP12 levels in cells that express FBXW7-R465C.

C-Met/Axl-IN-1 (Compound 22a) is an oral, selective type II c-Met/Axl inhibitor with IC50 values of 1 nM and 10 nM, respectively. It effectively suppresses tumor cell proliferation, induces cell cycle arrest, and apoptosis (apoptosis), showcasing potent anti-tumor activity.

SLF-amido-C2-COOH is a synthetic ligand for FKBP (SLF), and can be used in the synthesis of PROTACs.

Collismycin A, from Streptomyces, has antibacterial, antiproliferative, and neuroprotective effects. It inhibits various cancer cells and is iron-complexing.

Hypoxia inducer-1 (Compound N6) is a NO donor compound that is orally active and activated under hypoxic conditions. It exhibits high selectivity in releasing NO, inhibiting apoptosis, necrosis, and elevated levels of reactive oxygen species (ROS) associated with hypoxia. It modulates vasodilation and shows protective effects in a mouse model of myocardial hypoxic injury, making it useful for coronary heart disease research.

BY13 is an SRC-3 PROTAC degrader with a DC50 of 0.031 μM. It selectively obstructs the ER signaling pathway by downregulating ERα levels, showing greater selectivity over the androgen receptor (AR). BY13 effectively addresses endocrine resistance in breast cancer by inducing cell cycle arrest at the G1 phase and triggering apoptosis. Additionally, it surpasses Fulvestrant in efficacy and significantly inhibits the growth of resistant breast tumors in LCC2 xenograft mouse models, exhibiting no noticeable toxicity.

PD-L1/VISTA-IN-2 (Compound S8) is an orally active dual inhibitor targeting PD-L1 and VISTA, with an IC50 of 1.4 μM for PD-L1 and a KD of 2.1 μM for VISTA. This compound can activate the tumor immune microenvironment, exerting anticancer effects.

Src Inhibitor4 (Compound 18) is a derivative of KX-01 and functions as a Src inhibitor. It effectively disrupts tumor cells, damages microtubules, and induces cell cycle arrest, apoptosis, and immunogenic cell death. After introducing phenol or aniline functional groups, Src Inhibitor4 serves as a payload conjugation site for antibody-drug conjugates, showcasing antitumor activity.

Barakol, a primary compound found in Cassia siamea, inhibits MMP-3 activity and enhances the anti-metastatic effects of doxorubicin. Additionally, Barakol induces apoptosis (Apoptosis), generates reactive oxygen species, increases the Bax/Bcl-2 expression ratio, and activates caspase-9. This compound also exhibits laxative, anti-anxiety, central nervous system depressant, antioxidant, and anticancer properties.

Type-I/-II Photosensitizer-1 (compound 8b) is a photosensitizer with anticancer properties. It exhibits significant phototoxicity against A549 and 4T1 tumor cells. Under laser irradiation, Type-I/-II Photosensitizer-1 demonstrates strong oxygen-independent antitumor activity with an IC50 ranging from 1.50 to 1.76 μM.

Cuprichydroxide exhibits inhibitory activity against Ralstonia solanacearum and A549 cells and has acute pulmonary toxicity.

HSP90-IN-33 (compound 24e) is an effective Hsp90 inhibitor, demonstrating dissociation constants (Kd) of ≥200 µM for Hsp90α and 7.3 µM for Hsp90β. This compound induces cellular apoptosis (apoptosis) and arrests the cell cycle at the G0/G1 phase. Additionally, HSP90-IN-33 reduces the protein expression of ERα, CDK4, and Akt.

p38α inhibitor6 (compound 19) is a p38α inhibitor with an IC50 value of 0.68 μM. It induces apoptosis, arrests the cell cycle in the G0 and G2/M phases, reduces TNF-α concentration, upregulates the expression of the tumor suppressor gene p53, increases the Bax/BCL-2 ratio, and activates caspase3/7.

TOPOI/PARP-1-IN-2 (compound 6c) serves as a dual inhibitor targeting both PARP-1 and topoisomerase 1 (TOPO-1), with IC50 values of 32.2 nM and 46.2 nM, respectively. This compound exhibits greater selectivity for PARP-1 over PARP-2. Additionally, TOPOI/PARP-1-IN-2 disrupts the S phase of the cell cycle and induces apoptosis in the NCI-60 cancer cell lines.

2-deoxy-D-Glucose-13C6 is an internal standard for GC/LC-MS, a glycolysis inhibitor, and induces apoptosis in certain cells at 2 mg/ml.

[Au(L4)(CyJohnPhos)]SbF6 is a gold-containing compound that exhibits inhibitory effects on cyclooxygenase-1/2 (COX-1/2), suppresses the proliferation of colon cancer cells Caco2-/TC7 with an IC50 of 0.98 μM, and induces cell apoptosis (apoptosis). Additionally, [Au(L4)(CyJohnPhos)]SbF6 acts as an inhibitor of thioredoxin reductase (TrxR) and demonstrates antioxidative activity by modulating ROS levels.

Thalidomide-NH-(CH2)2-NH2 TFA is an alkyl-modified derivative of Thalidomide serving as a Cereblon ligand to recruit CRBN proteins and a pivotal intermediate in

BAY 1892005 is a p53 protein modulator that targets the p53 condenser for the study of diseases associated with misfolded p53 protein

MS78, an acetylation targeting chimera (AceTAC), specifically acetylates the p53Y220C mutant by recruiting the histone acetyltransferase p300/CBP.

Anticancer Agent 146 (Compound 1.19) acts as a necroptosis inducer and demonstrates anti-tumor efficacy in the MDA-MB-231 mouse xenograft model [1].

ECDD-S18 (compound ECDD-S18) induces apoptosis in a dose-dependent manner, effectively targeting the vacuolar ATPase (V-ATPase) and impairing lysosomal acidification.

Tubulin polymerization-IN-70 (compound Q19) is an effective inhibitor of tubulin polymerization. This compound exerts antiproliferative properties by targeting the colchicine binding site on tubulin, thereby inhibiting its polymerization. Tubulin polymerization-IN-70 also induces apoptosis and cell cycle arrest at the G2/M phase. Additionally, it triggers a decrease in mitochondrial membrane potential and elevates levels of reactive oxygen species (ROS). Moreover, Tubulin polymerization-IN-70 possesses anti-angiogenic and anticancer activities.

Apoptosisinducer 30 (Compound 15a) acts as an anticancer agent. It induces apoptosis in MCF-7 cells through the mitochondrial pathway. This compound elevates intracellular levels of reactive oxygen species (ROS), decreases mitochondrial membrane potential, and arrests the cell cycle at the G0/G1 phase. Apoptosisinducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and suppresses tumor growth in a mouse breast cancer model.

Quercetin-d3 hydrate, a deuterated form of Quercetin hydrate, acts as a flavonoid that stimulates recombinant SIRT1 and serves as a PI3K inhibitor. The compound specifically exhibits IC50 values of 2.4 μM, 3.0 μM, and 5.4 μM against PI3Kγ, PI3Kδ, and PI3Kβ, respectively.

Bfl-1-IN-5 (Compound (R,R,S)-26) is a selective inhibitor of Bfl-1, demonstrating an IC50 of 0.022 μM. This compound enhances the activity of caspase-3/7, with an EC50 of 0.37 μM, and also inhibits the viability of SU-DHL-1 cells, showing an EC50 of 1.3 μM.

Moracin N, a ferroptosis inhibitor derived from mulberry leaves, exhibits neuroprotective activity by mitigating oxidative stress [1].

Thalidomide-O-PEG2-propargyl is a cereblon-based E3 ligase ligand with a PEG linker for PROTAC-induced protein degradation.

LBM22, a CLK2 inhibitor, exhibits an IC50 value of 3.9 nM. It possesses anti-proliferative properties by inhibiting the phosphorylation of SR proteins. Additionally, LBM22 downregulates the expression of Wnt-related proteins and anti-apoptotic proteins, making it applicable in the study of non-small cell lung cancer.

CQ-ER is a Coumarin-quinazolinone-based photosensitizer targeting the endoplasmic reticulum (ER). It induces ferroptosis, thereby enhancing photodynamic therapy (PDT).

Tubulin polymerization-IN-72 (Compound 4a4) is a microtubule synthesis inhibitor with anticancer properties. By binding to the colchicine site, it disrupts the polymerization of tubulin, resulting in the arrest of cancer cells at the G2/M phase and inducing apoptosis (Apoptosis). The IC50 for its activity against cancer cells is 0.4-2.7 nM.

Narasin (sodium salt) (HainanMycin) induces tumor necrosis factor-related apoptosis-induced ligand (TRAIL)-mediated apoptosis by ER stress in glioma cells and

Anticancer agent 136 (compound 22), a C17-triazole analogue of Geldanamycin (GDM), exhibits an IC50 value of 3.38 μM against human dermal fibroblasts (HDF) and

STK17A/B-IN-1 hydrochloride is a potent, selective, orally active inhibitor of STK17A/B, displaying an IC50 value of 23 nM against STK17A. It is utilized in the research of tumors.

Caspase-3 activator 3 (compound 2h) effectively induces apoptosis in HL-60 and K562 cells by substantially activating caspase-3, demonstrating antileukemic

SZU-B6, a PROTAC degrader, targets and degrades SIRT6 with DC50 values of 45 nM in SK-HEP-1 cells and 154 nM in Huh-7 cells. It inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cell lines. Additionally, SZU-B6 induces apoptosis in SK-HEP-1 cells and causes cell cycle arrest at the G2/M phase. It demonstrates anti-tumor activity in murine models.

YCH3124 (compound Z33) is an inhibitor of USP7, exhibiting anti-tumor activity with an IC50 value of 41.9 nM. This compound demonstrates substantial in vitro anti-proliferative effects on various tumor cells, including LNCaP (IC50= 3.6 nM) and CHP-212 (IC50=9.9 nM). Moreover, YCH3124 induces apoptosis in CHP-212 cells by disrupting the cell cycle process during the G1 phase.

Siomycin A: thiopeptide antibiotic, selectively inhibits FOXM1, anti-tumor, induces apoptosis.

PRMT5-IN-45 (compound 36) is a potent and selective inhibitor of PRMT5, exhibiting an IC50 value of 3 nM. This compound effectively reduces the levels of symmetrical dimethylarginine (sDMA) and inhibits the proliferation of the MOLM-13 cell line by inducing apoptosis and causing cell cycle arrest.

EGFR-IN-131 (compound 3a) is an efficacious EGFR inhibitor capable of crossing the blood-brain barrier, with an IC50 value of 272.9 nM. This compound exhibits anti-proliferative activity, induces cellular apoptosis (apoptosis), and causes cell cycle arrest in the G0/G1 phase. Additionally, EGFR-IN-131 reduces the protein expression of p-EGFR.

Carubicin, an anthracycline antibiotic from Actinomadura carminata, disrupts DNA replication and repair by intercalating DNA and inhibiting topoisomerase II.

Fisetin quarterhydrate, a natural flavonol present in numerous fruits and vegetables, exhibits benefits including antioxidant, anticancer, and neuroprotective

Calcimycin (A-23187) is an antibiotic calcium ionophore that raises intracellular Ca2+ to induce cell death.

AMXT-1501 tetrahydrochloride is an inhibitor of polyamine transport.

Asaretoclax is an effective inhibitor of B-cell lymphoma 2 (Bcl-2), demonstrating potential for use in cancer research.

PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.

BK60106 is a selective and direct inhibitor of the transmembrane protein CD99, which causes cell death in Ewing Sarcoma cells.

c-Fos-IN-1 (Compound P16) acts as a c-Jun inhibitor, effectively reducing the mRNA and protein levels of c-Fos. It also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. This compound demonstrates anticancer properties through the inhibition of the ERK/c-Fos/Jun pathway. c-Fos-IN-1 curbs the proliferation and migration of gastric cancer cells, with an IC50 of 2.31 μM for MGC-803 cells, causing cell cycle arrest at the G2/M phase and inducing apoptosis in cancer cells. Additionally, c-Fos-IN-1 hampers the growth of gastric cancer tumors.

Photosensitizer-5, a photodynamic agent, exhibits cytotoxicity towards HeLa and HepG2 cells, with IC50 values of 10.4 nM and 6.9 nM, respectively. It induces cell death through lipid peroxidation via an iron-independent ferroptosis pathway. Additionally, Photosensitizer-5 displays antitumor activity in HeLa-tumor-bearing mice.

RIP2 Kinase Inhibitor 4, a selective RIPK2 PROTAC, degrades RIPK2 (pIC50=8), inhibits TNF-α release.

5-LOX-in-2: a 5-lipoxygenase inhibitor with IC50 of 0.33 μM, reduces kidney cancer cell activity, induces apoptosis.

Theophyllol (theophylline sodium acetate) can alter calcium levels in subcellular fractions of rat brain cortex.

BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL)

Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.

Anti-inflammatory agent 95 (Compound 2e) is a compound with potent anti-inflammatory properties, showing significant inhibition of NO production in LPS-induced RAW 264.7 mouse macrophages, with an IC50 of 8.8 μM. It also effectively suppresses the secretion of TNF-α and IL-1β, achieving inhibition rates of 60% and greater than 90% at 100 μM, respectively. Anti-inflammatory agent 95 holds promise for research into inflammatory diseases.

dMCL1-2 is a PROTAC-based MCL1 degrader, binding at 30 nM, and induces apoptosis in leukemia.

CDD-2807 is a serine/threonine kinase 33 (STK33) inhibitor with an IC50 of 9.2 nM. In mice, CDD-2807 demonstrates no significant toxicity and can cross the blood-testis barrier without accumulating in the brain. It offers reversible contraceptive effects, indicating potential for development as a male contraceptive.

ILS-920, a Rapamycin analog, has reduced immunosuppression, enhanced neuroprotection, and preferentially binds FKBP52 and L-type VGCC β1.

Apoptosisinducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer cells, demonstrating an IC50 of 12.8 μM and inducing early apoptosis in these cells. Additionally, it can bind to DNA molecules as well as Bax and Bcl-2 proteins, thereby inducing DNA damage.

MK-4166 is a humanized IgG1 agonistic monoclonal antibody targeting GITR. It is capable of enhancing the proliferation of both naive T lymphocytes and tumor-infiltrating T lymphocytes.

PERK-IN-6 is a novel and highly potent PERK inhibitor (IC50:2.5 nM).

MD-265 is a PROTAC degrader that targets and degrades MDM2, leading to the activation of p53 in cancer cells with wild-type p53. MD-265 achieves complete tumor regression and enhances long-term survival in leukemic mice.

Bleomycin A5, or Pingyangmycin, is an oral glycopeptide antibiotic and acts as an antineoplastic and apoptosis inducer.

Prodigiosin is a secondary metabolite of Symbiotic bacteria. It also has anti-fungal and anti-cancer activity.

KGYY15 (Mouse KGYY15), a peptide that targets CD40, exhibits weak inhibition of the CD40-CD40L interaction, with an IC50 exceeding 1 mM. At a concentration of 100 μM, KGYY15 activates the NF-κB pathway by 33%.

Tubulin polymerization-IN-45, a tubulin-targeting agent, acts as a tubulin polymerization inhibitor by binding to the tubulin's colchicine site.

5-Methoxysterigmatocystin is a mycotoxin characterized by its cytotoxic and genotoxic properties. It exhibits cytotoxic effects on cancer cell lines A549 and HepG2, with IC50 values of 5.5 μM and 0.7 μM, respectively. Additionally, it induces DNA damage. 5-Methoxysterigmatocystin acts as a photosensitizer, generating singlet oxygen (1O2) under visible light.

PROTACERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader designed to diminish estrogen receptor α (ERα) and aromatase (ARO). It demonstrates a Ki of 0.25 μM for ERα binding and an IC50 of 4.6 μM for ARO inhibition. This compound curbs proliferation in wild-type MCF-7 cells (IC50=0.54 μM) and ERα mutant variants MCF-7EGFR (IC50=0.075 μM), MCF-7D538G (IC50=0.31 μM), and MCF-7Y537S (IC50=2.3 μM), while also downregulating ERS1 and MYC expression. PROTACERα Degrader-9 arrests the cell cycle at the G2/M phase and induces apoptosis in MCF-7 cells, exhibiting antitumor efficacy in mouse models.

Boanmycin, an antibiotic exhibiting antitumor activity, induces cellular senescence and apoptosis [1] [2] [3].

PARP1-IN-27 (Compound 9B) serves as an inhibitor of both PARP1 and PARP2, exhibiting IC 50 values of 2.53 nM and 6.45 nM, respectively, in SUM149PT cells. This compound effectively suppresses the proliferation of BRCA-mutated cancer cell lines such as SUM149PT, HCC1937, and Capan-1, with respective IC 50 values of 0.62, 1.91, and 4.26 μM. Additionally, PARP1-IN-27 exacerbates DNA double-strand breaks, enhances ROS production, causes G2/M phase cell cycle arrest, and triggers apoptosis in SUM149PT cells.

Destruxin B: cyclic peptide from Metarhizium fungus, induces apoptosis in lung cancer via mitochondrial pathway.

UZH1a: METTL3 inhibitor, IC50 280 nM, used for epitranscriptomic modulation and has antitumor properties.

Apoptosis Inducer 3 (Compound 3), a selective apoptosis triggering agent, induces both apoptosis and late-apoptosis phases, demonstrating cytotoxic effects

FHD-286 is an inhibitor of BRM/BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.

12-Deoxyphorbol 13-palmitate, a monomer derived from the roots of Euphorbia fischeriana, exhibits notable antitumor activity. This compound induces cell cycle arrest and apoptosis in gastric cancer cells by modulating key cell cycle regulators, such as cyclin B, cyclin A, and CDC2. Additionally, 12-Deoxyphorbol 13-palmitate significantly diminishes liver fibrosis by targeting APOL2 and impairing the APOL2–SERCA2–PERK–HES1 signaling pathway.

Sarglaroids F (compound 6), an anti-inflammatory agent extracted from the roots of Grass Coral, suppresses LPS/ATP-induced IL-1β secretion by modulating K+

Marstacimab (PF-06741086) is a neutralizing antibody that binds and inhibits human tissue factor pathway inhibitors.

Ferroptosisinducer-4 (Compound 5) is a phospholipid-based ferroptosis inducer featuring a terminal double bond at the sn-2 position. It exhibits significant cytotoxicity towards HT-1080 cells with an IC50 value of 18 μM. The toxicity mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane induced by the terminal double bond. Ferroptosisinducer-4 can be utilized in studies pertaining to the regulation of ferroptosis.

Minocycline is a useful organic compound for research related to life sciences. The catalog number is T131626 and the CAS number is 10118-90-8.

YL5084 is a selective JNK2/3 inhibitor with IC50s: JNK2 (70 nM), JNK3 (84 nM), and antiproliferative, apoptosis-inducing effects.

5,10,15,20-Tetrakis(4-methoxyphenyl)porphyrin is a capable of forming complexes with metal ions and exhibit phototoxicity towards Hep-2 cells.

CPTH2 is an inhibitor of the HAT activity of Gcn5.

TopoisomeraseI inhibitor 17 (Compound 7h) is an inhibitor of TopoisomeraseI (Top1). It reduces DDX5 and reverses the locking effect of DDX5 on Top1 activity. This compound induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. It triggers apoptosis by decreasing anti-apoptotic proteins XIAP, Bcl-2, and Survivin, while increasing pro-apoptotic proteins Bax and γH2AX. Moreover, TopoisomeraseI inhibitor 17 halts progression at the G2/M checkpoint, leading to cell cycle arrest. It significantly impairs colorectal cancer cell colony formation and migration, and effectively reduces tumor size in human PDX tumor mouse models.

Compound 7, also known as RAR/RXR agonist-1, is a chlorinated isomer of retinoic acid and acts as a selective RARα agonist and a partial RXRα agonist. It is capable of activating RXRα, thereby inducing G2/M arrest and apoptosis in cancer cells.

Monactin is a Marcrotetrolide antibiotic produced by cycloheximide producing species of Streptomyces. It is a homolog of nonactin from the same species.

Dynorphin A TFA: endogenous peptide, potent KOR agonist, affects CNS, involved in neuron death research.

AlPcS2 disodium: a photosensitizer for cancer therapies, isomeric mix, and used as a dye, reagent, and luminescent agent.

PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.

Tomatine hydrochloride halts fungi/bacteria growth, is extracted from wild tomato leaves, and precipitates steroids.

7-Methoxy-1-tetralone may have insecticidal activity.

Cefatrizine inhibits eEF-2 kinase, affecting apoptosis, autophagy, and ER stress in cancers.

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.

FLT3-IN-29 (Compound MY-10) is an FLT3 inhibitor with IC50 values of 6.5 nM and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants, respectively. It induces cell cycle arrest at the G0/G1 phase and effectively triggers apoptosis (Apoptosis). Additionally, FLT3-IN-29 reduces reactive oxygen species (ROS) and mitochondrial membrane potential (MMP), displaying anti-leukemic properties.