nude

Inobrodib (CBP-IN-1) is a potent inhibitor of p300/CBP bromodomain.

V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively targets the amino acid transporter ASCT2 (SLC1A5) without affecting ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake in HEK-293 cells (IC50=9.6 μM). V-9302 can be used for research on tumor and amino acid transport

FGFR1/DDR2 inhibitor 1 is an inhibitor of discoidin domain receptor 2 (DDR2) and fibroblast growth factor receptor 1 (FGFR1), with IC50 values of 31.1 nM, 108.4 nM, and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

MYCMI-6 (NSC-354961) is a potent and selective inhibitor of endogenous MYC:MAX protein interactions,reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without severe side effects.

Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, with KDs of 0.2, 0.76, 13, and 1.2 nM for EGFR, HER2, BLK, and RIPK2, respectively, and exhibits anticancer activity.

Oxiconazole nitrate (Ro 13-8996) is the nitrate salt form of oxiconazole, a broad-spectrum imidazole derivative with antifungal activity. Likely inhibiting cytochrome P450-dependent demethylation of lanosterol, it prevents ergosterol synthesis, a crucial component of the fungal cell membrane. This disruption of membrane synthesis and integrity alters permeability, promotes loss of essential intracellular components, and inhibits fungal cell growth.

J-104871 (UNII-6137X5QNJF) is a novel farnesyltransferase (FTase) inhibitor that competitively blocks Ras farnesylation in vivo, inhibits Ras processing in activated H-ras-transformed NIH3T3 cells, and suppresses tumor growth in nude mice transplanted with activated H-ras-transformed NIH3T3 cells.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK/p38 MAPK signaling pathways in the murine macrophages.

Tubulin polymerization-IN-68 (compound 32) serves as a tubulin inhibitor, disrupting cellular microtubule networks by hindering tubulin polymerization. It also upregulates PARP-1 and caspase-3 expression, thereby inducing apoptosis and exhibiting anticancer properties. Notably, Tubulin polymerization-IN-68 effectively suppresses HepG2 cells with an IC50 of 93 nM and markedly reduces the growth of HepG2 xenograft tumors in nude mice through oral administration.

PRDX1-IN-3 (SOMCL-19-048) is a PRDX1 covalent inhibitor with anti-colorectal cancer activity. PRDX1-IN-3 can effectively inhibit the proliferation of colorectal cancer cells and significantly reduce the anti-tumor effect on colorectal cancer nude mice carrying PRDX1 gene knockout. PRDX1-IN-3 can also upregulate downstream genes of the p53 signaling pathway and exert anti-cancer effects.

Δ8-Tetrahydrocannabinoquinone (HU-336) is a potent anti-angiogenic agent that inhibits angiogenesis by directly inducing apoptosis in vascular endothelial cells. It achieves this without altering the expression of pro-angiogenic and anti-angiogenic cytokines and receptors. Δ8-Tetrahydrocannabinoquinone also shows significant effectiveness against tumor xenografts in nude mice.

WRN inhibitor 14 (compound S35) is an orally administered WRN inhibitor with anticancer properties. It effectively suppresses tumor growth in the SW48 xenograft model in BALB/c nude mice.

TrxR1 prodrug-1 (compound 5u) is a potent inhibitor of TrxR1, demonstrating significant antitumor activity in nude mice and NSCLC organoids.

SGK1-IN-6 (compound 12f) is an SGK1 inhibitor with an IC50 value of 0.39 μM. In PC3 xenograft models using BALB/c nude mice, SGK1-IN-6 effectively hinders tumor growth without causing any observable toxicity.

PROTACGPX4 degrader-4 is a GPX4 PROTAC degrader with a DC50 of 5.32 nM. It inhibits the activity of cancer cell lines RT4, T24, and J82 with IC50 values of 0.09, 2.97, and 7.58 μM, respectively. This compound elevates lipid ROS levels and induces ferroptosis in T24 and RT4 cells. In T24 tumor-bearing BALB/c nude mouse models, PROTACGPX4 degrader-4 demonstrates antitumor activity. It is applicable to bladder cancer research.

SDX-7539 is a selective MetAP2 inhibitor that inhibits the proliferation of HUVEC, with an IC50 of 120 μM. It has demonstrated antitumor activity in xenografted NSCLC in athymic nude mice.

PROTACERα Degrader-11 is a selective ERα PROTAC degrader with intrinsic fluorescence (Ex: 366 nm, Em: 440 nm). It demonstrates strong anti-proliferative activity, selective ERα degradation, and fluorescence imaging capability in the MCF-7 breast cancer cell line. PROTACERα Degrader-11 induces G2/M phase arrest and apoptosis in MCF-7 cells. In athymic nude mice, it shows good safety with no acute toxic reactions at a dose of 500 mg/kg. PROTACERα Degrader-11 is suitable for breast cancer research.

eIF4E/eIF4G PPI-IN-1 is an inhibitor that disrupts the interaction between eIF4E and eIF4G, exhibiting a dissociation constant (KD) of 20.2 μM for the eIF4E protein. It demonstrates antitumor effects through various mechanisms, including modulation of eIF4E activity via inhibition of the Ras/MAPK/eIF4E signaling pathway, influencing apoptosis and cell migration. Additionally, eIF4E/eIF4G PPI-IN-1 inhibits the growth of HepG2 xenografted tumors in nude mice and is relatively non-toxic to mice.

Tubulin-IN-51 is an orally active tubulin inhibitor with an IC50 of 31 nM. It promotes tubulin polymerization in vitro and does not competitively bind with Paclitaxel. Tubulin-IN-51 inhibits the binding of Vinblastine to tubulin and suppresses tumor growth in various nude mouse xenograft models, including those using A549 human non-small cell lung cancer (NSCLC) cells and U87-MG human glioblastoma.

ROR1-IN-4 is a selective inhibitor of ROR1 with a dissociation constant (Kd) of 52 nM. It exhibits potent antiproliferative activity in the triple-negative breast cancer (TNBC) cell line MDA-MB-231, with an IC50 of 75 nM. ROR1-IN-4 reduces colony formation, induces apoptosis (apoptosis), and inhibits phosphorylation of ROR1(Tyr786) in these cells. Additionally, ROR1-IN-4 demonstrates significant antitumor efficacy in nude mice bearing subcutaneous MDA-MB-231 xenograft tumors. This compound is applicable for research related to TNBC.

D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) [Ins(1,3,4,5,6)P5 (ammonium salt)] is an isomer of inositol phosphate that functions as a small, soluble second messenger in cellular signaling. It can bind to the PH domain of Grp1 with a dissociation constant (Kd) of 590 nM. This compound inhibits the phosphorylation and kinase activity of Akt/PKB, leading to apoptosis in ovarian, lung, and breast cancer cells. Additionally, it exhibits anti-angiogenic activity in vitro, blocking capillary formation by HUVECs, and demonstrates antitumor effects in cancer xenograft models in nude mice.

D574-0246 is a dual-active inhibitor of OXCT1, targeting the enzyme's keto-dehydrogenase and succinyl-transferase activities. It reduces substrate-specific (LACTB K284) and global protein succinylation in HepG2 cells and lowers the ketolytic activity of OXCT1. The compound decreases the viability of HCC cells with an IC50 of 16.49 μM in PLC cells and 6.656 μM in HepG2 cells. In nude mice with HepG2 xenograft tumors overexpressing OXCT1, D574-0246 demonstrates anti-tumor effects. It is applicable for studies on hepatocellular carcinoma (HCC).

Ferroptosisinducer-12 is a potent and selective inducer of ferroptosis. It demonstrates strong antiproliferative activity against HT1080 and OS-RC-2 cell lines, with IC50 values of 3 nM and 5 nM, respectively. This compound significantly inhibits GPX4 enzyme activity, induces intracellular ROS, and elevates Fe2+ levels within OS-RC-2 cells. Moreover, Ferroptosisinducer-12 markedly inhibits tumor growth in BALB/c nude mice bearing OS-RC-2 xenografts. It is applicable for cancer research.

MMP-2/9-IN-2 (Compound 6k) functions as an inhibitor of MMP-2 and MMP-9, with IC50 values of 29.27 μM and 24.87 μM, respectively. It exhibits selective toxicity against various human liver cancer cell lines and induces cell cycle arrest and apoptosis (apoptosis), significantly inhibiting cell migration and invasion. Additionally, MMP-2/9-IN-2 suppresses the phosphorylation of the STAT3 signaling pathway and demonstrates potent antitumor activity in a nude mouse xenograft model with HepG2 liver cancer cells.