cancer targeting compound 1

Cancer-Targeting Compound 1 can be used in the study of hormone-related cancers, including the treatment or prevention of fibroids, uterine leiomyomas, polycystic ovarian syndrome, or hormone-dependent Cancer, among others.

NPS ALX Compound 4a hydrochloride(1:1) is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM.

Antimicrobial Compound 1 is an alkyl pyridinium compound with Tail 12C, Head 4-carboxyl. Antimicrobial Compound 1 exhibits antimicrobial activities against B. subtilis and E. coli.

Itch-Targeting Compound 1 is an anti-itch compound. It is effective in preventing or treating reactions on insect's bites, reactions on environmental allergens, skin infections, external vermination, or itches occurring in renal dialysis patients.

Antiasthmatic Compound 1 is an antiasthmatic agent.

Antibacterial compound 1 is an antibacterial compound.

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) (PIK-III analogue) is a potent and selective inhibitor of VPS34( IC50 : 15 nM)

(Rac)-Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor.

Compound SC-1 is a a derivative of the multiple tyrosine kinase inhibitor sorafenib. Compound SC-1 potently inhibits the phosphorylation of STAT3 by blocking STAT3 phosphorylation and activation, and induces apoptosis in hepatocellular carcinoma cell lines[1].

Urinary Incontinence-Targeting Compound 1, used in the research of urinary incontinence, is a sulfonanilide derivative.

Arrhythmias-Targeting Compound 1 is a compound. It is used in the research of arrhythmias.

Neurodegenerative Disorder-Targeting Compound 1 is an inhibitor of calpain [1].

Asthma relating compound 1 is an anti-asthmatic compound.

Neuromuscular-targeting compound 1 can be used to study muscular dystrophy and neuromuscular-related diseases.

Neuromuscular Disorder-Targeting Compound 1 is a compound used in the research of neuromuscular disorders, for example, symptoms of chronic fatigue syndrome and fibromyalgia syndrome.

Arrhythmic-Targeting Compound 1 is used for arrhythmic disease, with nitrogen-containing spirocycles.

PBRM1-BD2-IN-7, a selective and cell-active inhibitor targeting the polybromo-1 (PBRM1) bromodomain, demonstrates inhibitory efficacy against PBRM1-BD2 with an IC50 value of 0.29 μM. This compound is utilized in cancer research.

PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.

mTOR/HDAC-IN-1 (Compound 50) is a dual inhibitor targeting both mTOR and HDAC with respective IC50 values of 0.49 nM and 0.91 nM. It holds potential as an anti-cancer agent [1].This compound is unstable in powder form and other related salt forms are recommended.

TCIP 1 is a small molecule in the category of transcriptional/epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].

Tubulin/JAK2-IN-1 (compound 7g) serves as a potent dual inhibitor targeting both Janus kinase 2 (JAK2) and microtubules, demonstrating significant antiproliferative effects against cancer cells [1].

BT8009 is a conjugate targeting Nectin-4, demonstrating a dissociation constant (Kd) of 2.5 nmol/L for the hNectin-4 ECD. This compound comprises a Nectin-4-specific bicyclic peptide, a cleavable linker, and MMAE. It is applicable in the study of advanced and metastatic urothelial cancer [1].

LIN28-IN-1 (compound 5) is a selective inhibitor targeting the RNA-binding protein LIN28, specifically binding to its cold shock domain (CSD). This compound robustly interrupts the LIN28-let-7 miRNA interaction with an IC 50 of 5.4 μM, thereby mitigating LIN28's adverse effects on epigenetic gene control. Furthermore, LIN28-IN-1 exhibits significant anti-proliferative activity against LIN28-expressing JAR cancer cells, evidenced by an IC 50 value of 6.4 μM [1].

Eciskafusp alfa, a cis-targeted IL2v immunocytokine, acts on programmed cell death 1 (PDCD1, commonly known as PD-1), preferentially targeting antigen-specific stem-like PD-1+ TCF-1+ CD8+ T cells to differentiate into a more effective effector population. This compound is applicable in the study of cancer and chronic infections [1].

QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.

hCA/Wnt/β-catenin-IN-1 (Compd 15) serves as an inhibitor with selective affinity for hCA isoforms II, IX, and XII, exhibiting K i values of 33.6, 24.1, and 6.8 nM, respectively. Additionally, this compound attenuates P-gp activity and impedes the Wnt/β-catenin signaling pathway. Furthermore, it compromises the viability of cancer cells, specifically targeting the NCI/ADR-RES DOX-resistant cell line [1].

LEB-03-146, a WEE1 DUBTAC (deubiquitinase-targeting chimera), effectively links AZD1775 (Adavosertib) with the OTUB1 recruiter EN523 via a PEG2 linker. This compound demonstrates considerable WEE1 stabilization in HEP3B hepatoma cancer cells [1].

BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL) and the AR-V7 splice variant. It specifically antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor), prompting apoptosis in prostate cancer (PC) cells. In LNCaP xenograft models, BWA-522 demonstrated tumor growth inhibition (60 mg/kg, po; TGI=76%). The compound effectively reduced levels of AR-V7 and AR-FL by 77.3% at 1 μM and 72.0% at 5 μM, respectively, in VCaP and LNCaP cell lines [1].

AZ'6421, functioning as a Proteolysis Targeting Chimera (PROTAC), selectively degrades estrogen receptor alpha, demonstrating potent anti-tumor activity by inhibiting uncontrolled cellular proliferation characteristic of malignant diseases. This compound holds promise for cancer research, including breast cancer applications [1].

IDO1/TDO-IN-6 (compound 11) is a dual inhibitor targeting IDO1 and TDO, exhibiting IC50 values of 2.25 μM for IDO1 and 2.89 μM for TDO. The compound further demonstrates Ki values of 1.9 μM for IDO1 and 3.1 μM for TDO, marking its potential utility in cancer and immunology research [1].

PROTAC EGFR degrader 7 (compound 13b) is a potent, selective CRBN-recruiting agent targeting EGFR L858R/T790M mutations with a DC50 of 13.2 nM. It effectively inhibits proliferation in NCI–H1975 cells with an IC50 of 46.82 nM and significantly triggers apoptosis and G2/M phase arrest in these cells. Demonstrating antitumor efficacy, PROTAC EGFR degrader 7 holds promise for non-small cell lung cancer (NSCLC) research [1].

Targaprimir-96 TFA, a potent inhibitor of microRNA-96 (miR-96) processing, selectively reduces miR-96 production in cancer cells, thereby inducing apoptosis. This compound exhibits low nanomolar affinity binding to primary miR-96 (pri-miR-96), targeting it specifically in breast cancer cells while remaining inactive in normal breast cells [1].

EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.092 μM for HER2, respectively. Moreover, it demonstrates inhibition of DHFR with an IC50 of 0.193 μM. Notably, this compound induces cell cycle arrest in the S phase and triggers apoptosis in MCF7 breast cancer cells [1].

WRN Inhibitor 1 (example 7) is an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN), selectively targeting its helicase domain. This compound is potentially useful for cancer research [1].

MS9715 is a potent and selective NSD3-targeting PROTAC, designed by leveraging BI-9321, which targets the PWWP1 domain of NSD3, in conjunction with an E3 ligase VHL ligand. This compound holds potential for research in NSD3-dependent cancer treatments [1].

HDAC1/CDK7-IN-1 (compound 8e) serves as a dual inhibitor targeting both CDK7 and HDAC1, with IC50 values of 893 nM and 248 nM , respectively. This compound effectively suppresses the proliferation of various cancer cell lines, including MDA-MB-231, MCF-7, A549, and HCT-116. Additionally, it triggers cell cycle arrest and apoptosis in HCT-116 cells and impedes their migration [1].

EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor targeting EGFR and CDK-2, demonstrating IC50 values of 89.6 nM for EGFR and 165.4 nM for CDK-2. It prompts apoptosis in MCF-7 cells and causes S phase cell cycle arrest, exhibiting substantial anti-cancer activity with an IC50 of 2.74 μM against MCF-7 cells [1].

GXF-111, a proteolysis targeting chimera (PROTAC) molecule, efficiently induces the selective degradation of the BRD3 and BRD4-L proteins. It exhibits high binding affinities to both BRD3 BD1 and BRD3 BD2, with K i values of 11.97 nM and 2.35 nM, respectively. This compound is utilized in cancer research [1].

PTK7/β-catenin-IN-1 (compound 01065) is a potent inhibitor targeting PTK7/β-catenin and p53/MDM2, with IC50 values of 8.9 μM and 56.5 μM, respectively. This compound shows promise for cancer research applications [1].

CFI-402257 hydrochloride, a highly selective and orally bioavailable inhibitor targeting TTK/Mps1, demonstrates an in vitro IC50 value of 1.7 nM against TTK. This compound exhibits anti-cancer activity [1].

VEGFR-2/DHFR-IN-2 (compound 5b) is a dual inhibitor targeting VEGFR-2 and DHFR, with respective IC50 values of 0.623 μM and 9.085 μM. It demonstrates potent cytotoxicity against C26, HepG2, and MCF7 cancer cell lines, with IC50 values ranging from 3.59 μM to 8.38 μM. VEGFR-2/DHFR-IN-2 holds promise for cancer research [1].

Sulfisoxazole diethanolamine, also known as Sulfafurazole diethanolamine, is a sulfonamide antibacterial compound with an oxazole substituent. It acts as an endothelin receptor antagonist, specifically targeting endothelin receptor A with an IC50 value of 0.60 μM and endothelin receptor B with an IC50 value of 22 μM. Additionally, Sulfisoxazole diethanolamine has been found to inhibit the release of breast cancer exosomes by specifically targeting endothelin receptor A [1] [2].

SIRT1/2/3-IN-1 (compound 10) is a potent, selective, and cell-permeable inhibitor targeting SIRT1, SIRT2, and SIRT3, demonstrating inhibitory concentrations (IC50s) of 0.54 μM, 0.253 μM, and 0.72 μM, respectively. It is utilized in cancer research [1].

ADH-6 TFA, a tripyridylamide compound, effectively disrupts the self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD, thereby targeting and disassociating mutant p53 aggregates in human cancer cells. This action restores the transcriptional activity of p53, resulting in cell cycle arrest and apoptosis. Consequently, ADH-6 TFA holds potential for cancer research [1].

Zalutumumab, a fully human IgG1 monoclonal antibody, exhibits high affinity for the epidermal growth factor receptor (EGFR), selectively targeting its domain III. It functions by inhibiting the binding of the epidermal growth factor (EGF) and obstructing the receptor's active conformation through steric hindrance. With EC50 values of 7 nM for its IgG and 19 nM for the Fab fragment, Zalutumumab demonstrates potent interaction capabilities. This compound is primarily utilized in cancer research [1] [2] [3].

Cantuzumab mertansine (SB-408075; huC242-DM1), an antibody-drug conjugate (ADC), comprises the potent maytansine derivative (DM1) linked to the humanized monoclonal antibody (huC242) targeting CanAg. Demonstrating cytotoxicity against colon cancer cells, this compound shows extensive antitumor effectiveness across various CanAg-positive human tumor xenografts [1] [2].

VEGFR-2/DHFR-IN-1 (compound 8b) is a chemical inhibitor targeting VEGFR-2 and DHFR, exhibiting IC50 values of 0.384 μM and 7.881 μM, respectively. It demonstrates effective antibacterial properties against a range of pathogens including Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA, with MIC values ranging from 8 to 16 μg/mL. Additionally, this compound shows potent cytotoxic effects against various cancer cell lines such as C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM, rendering it a valuable tool for cancer research [1].

JET-209 is a potent proteolysis-targeting chimera (PROTAC) that effectively degrades CBP/p300, exhibiting half-maximal degradation concentration (DC50) values of 0.05 nM for CBP and 0.2 nM for p300. The compound comprises lenalidomide (the cereblon ligand), a connecting linker, and GNE-207 (the bromodomain inhibitor). JET-209 is utilized in cancer research [1].

Anticancer Agent 143 (Compound 369), a potent dual inhibitor targeting PTPN2 and PTP1B, exhibits IC50 values below 2.5 nM. It is employed in cancer research [1].

ALK2-IN-5, a pyrazolopyrimidine compound, serves as an inhibitor of ALK2 and FGFR, targeting disorders linked with their activity, including cancer [1].