Cytoskeletal Signaling

<p>A unique collection of 263 kinase inhibitors/regulators for specific targeting of kinases, ready for high-throughput screening and high-content screening.</p>

<p>Vinzolidine is a semi-synthetic vinca alkaloid. It exerts cytotoxic effects on tumor cells by inhibiting cell division through disruption of tubulin polymerization. Vinzolidine can be utilized in research to investigate synergy with other chemotherapy or biotherapy drugs, as well as cancer cell tolerance or resistance, and to explore strategies to overcome these challenges.</p>

<p>2-Methylbutyrylcarnitine (chloride) acts as a gut microbial metabolite that targets integrin α2β1 on platelets, facilitating the activation of cytosolic phospholipase A2 (cPLA2) and enhancing platelet hyperresponsiveness. This compound further augments platelet hyperreactivity and promotes thrombus formation in mice. It is also characterized as a branched-chain acylcarnitine.</p>

<p>TTBK1-IN-2, a TTBK1 inhibitor with IC50s of 0.24/4.22 µM, lowers TDP-43 phosphorylation in vitro and in mice.</p>

<p>αvβ5 integrin-IN-1, a potent and selective αvβ5 integrin inhibitor, exhibits a high inhibitory potency with a pIC50 value of 8.2.</p>

<p>AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.</p>

<p>PDK-IN-1, a PDK inhibitor, IC50: 0.03μM (PDK1), 0.1μM (HSP90), reduces tumor mass.</p>

<p>Anti-α-Tubulin Antibody, AF555 conjugate, is a mouse-derived monoclonal antibody conjugated with the red fluorescent dye Alexa Fluor 555, designed for the</p>

<p>Fuzapladib (IS-741) is a PLA2 inhibitor that reduces Mac-1 expression to prevent inflammation and pancreatitis.</p>

<p>MPH-220: Oral myosin-2 inhibitor, induces muscle relaxation, useful for spasticity research.</p>

<p>KQAGDV is a fibrinogen γ-chain cell adhesion peptide, targeting α2bβ3 integrin, and binds SMCs.</p>

<p>KT D606 is a PAK kinase family inhibitor with an IC50 of 4 μM. It selectively inhibits the proliferation of cancer cells transformed by oncogenic RAS mutants, making it useful for studying RAS/PAK1-induced cancers.</p>

<p>Ac-MRGDH-NH2 is a pentapeptide containing the RGD sequence. It is utilized in the synthesis of the diastereomeric prodrugs Λ- and Δ-[Ru(Ph2phen)2(κS,κN-(Ac-MRGDH-NH2))]Cl2. In these prodrugs, Ac-MRGDH-NH2 serves as a photolabile protecting group for the cytotoxic diruthenium aqua complexes [Ru(Ph2phen)2(OH2)2]2+, offering integrin targeting and photoactivation properties. Consequently, Ac-MRGDH-NH2 can be applied in studies exploring tumor-targeted photoactivatable chemotherapy.</p>

<p>T-808 is a tau tracer which may be used in radiographic labeling of Tau aggregates during Alzheimer's disease.</p>

<p>H-7: potent PKC inhibitor with 6 μM Ki, also blocks cyclic nucleotide-dependent kinases.</p>

<p>Modified MMAF, an ADC cytotoxin, aids in ADC synthesis for targeted cancer research.</p>

<p>Coronaridine is a useful organic compound for research related to life sciences. The catalog number is T124824 and the CAS number is 467-77-6.</p>

<p>PROTAC BP3 selectively degrades HSP90, inhibits breast cancer growth (DC50=0.99µM), CRBN-dependent.</p>

<p>IIQLPEIVVV TFA serves as a specific inhibitor targeting the Drp1-Mff interaction. This compound discriminates between physiological and pathological fission, hindering physiological fission which leads to mitochondrial dysfunction. IIQLPEIVVV TFA is also utilized in research related to Huntington's disease.</p>

<p>αVβ8-IN-1 is an αVβ8 integrin inhibitor that suppresses the growth of multiple tumour cell lines (EMT6, CT26, KPC, TKCC-10).</p>

<p>PDI-IN-4 (Compound 14d) is a protein disulfide isomerase inhibitor with an IC50 value of 0.48 μM. It prevents platelet aggregation and thrombosis by reducing the activation of GPIIb/IIIa, without causing significant cytotoxicity. PDI-IN-4 is applicable in thrombosis research.</p>

<p>Microtubule-associated protein tau (26-44) is a synthetic peptide with an amino group conjugated to glutamine and a carboxyl group conjugated to lysine.</p>

<p>17-DMAP-GA, a Geldanamycin analogue, acts as an HSP90 inhibitor, leading to cell cycle abnormalities.</p>

<p>LY 379196, a potent PKC-β inhibitor (IC 50: 50 nM for PKC βI and 30 nM for PKC βII), effectively suppresses the proliferation of bovine retinal microvascular endothelial cells (BREC) induced by VEGF, IGF-1, and bFGF. This compound serves as an antiproliferative agent for proliferative retinopathy.</p>

<p>Compound H26, a derivative of corosolic acid, functions as Hypoglycemic agent 3. It exhibits lipid-lowering and significant blood glucose-reducing properties, making it a potential hypoglycemic drug. Hypoglycemic agent 3 targets MCCC1 to mitigate insulin resistance, and may be useful in researching type 2 diabetes.</p>

<p>GRGDSPK (EMD 56574) is an inhibitory peptide for RGD-mediated adhesion between integrin and extracellular matrix molecules.</p>

<p>Tubulin polymerization-IN-48 (Compound 4k) is an inhibitor of tubulin polymerization, moderately disrupting the microtubule network.</p>

<p>BCR-ABL-IN-3 irreversibly inhibits Bcr-Abl with &lt;100 nM IC50, showing significant anti-cancer effects.</p>

<p>Tubulin Inhibitor 37 (Compound 12) effectively impedes tubulin aggregation (IC50 = 1.3 µM) and demonstrates antiproliferative activity against human tumor cell</p>

<p>"hBChE-IN-1, a quinolizidine, potently inhibits hBChE (IC50=7nM), selective over hAChE, and blocks tau and Aβ 40 aggregation for Alzheimer's research."</p>

<p>NU074381b (compound 5b) is an effective inhibitor of S100A4, disrupting the formation of the S100A4-NMII complex with an IC50 value of 0.48 µM. Additionally, it inhibits cell proliferation and migration.</p>

<p>AKT Kinase Inhibitor HCl is an Akt inhibitor with antitumor activity.</p>

<p>Rotigaptide, modulates Cx43 for gap junctions, counteracts uncoupling, and maintains communication under stress.</p>

<p>GSK3178022 is a human IgG1 monoclonal antibody (mAb) that targets LRP6. It inhibits the expression of the WNT target genes SP5 and AXIN2 and demonstrates antitumor activity in colorectal cancer RSPO fusion models. The recommended isotype control is HumanIgG1kappa, Isotype Control.</p>

<p>PROTAC BCR-ABL Degrader-1 (compound PROTAC 1), featuring a 2-oxoethyl linker, promotes Bcr-Abl degradation through the ubiquitin-proteasome pathway and</p>

<p>Crosstide is a peptide analog of glycogen synthase kinase-3 (GSK-3) that functions as a natural substrate for Akt/PKB.</p>

<p>Pironetin, from Streptomyces, inhibits microtubule polymerization and tumor growth, and causes cell cycle arrest.</p>

<p>ALB-109564 dihydrochloride: Semi-synthetic, vinblastine-derived, microtubule inhibitor, arrests tumor cells in G2/M phase.</p>

<p>Catumaxomab is a rat-mouse hybrid lgG2 monoclonal and bispecific antibody that binds to the antigens CD3 and EpCAM for malignant ascites in cancer patients.</p>

<p>BIO5192 hydrate: potent α4β1 inhibitor, binds selectively (Kd&lt;10 pM, IC50=1.8 nM), boosts murine HSPC mobilization 30x.</p>

<p>Tubulin inhibitor 48 (compound 16) is an anticancer agent targeting microtubules. It exhibits IC50 values of 0.1 μM and 0.07 μM against LN-229 and Capan-1 cells, respectively.</p>

<p>BMP Agonist 1 (compound 2 b) is a small-molecule stimulator of bone morphogenic protein (BMP) signaling, crucial for the differentiation of C2C12 cells.</p>

<p>Synthetic peptide analog of bovine myelin basic protein (MBP). Non-competitive inhibitor of PKC (IC50 = 28 - 62 mM).</p>

<p>Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI) exhibiting antiproliferative activity against the chronic myeloid leukemia (CML) cell line K562, with a CC50 of 0.8 µM. Tyrosine kinase-IN-8 is applicable for research in chronic leukemia.</p>

<p>cSRC/BCR-ABL1-IN-1 (compound 16a) is a dual-target inhibitor of the cSRC/BCR-ABL1 kinases.</p>

<p>hAChE-IN-1 (Compound 24) is a potent inhibitor of human acetylcholinesterase (hAChE), exhibiting an inhibition concentration half-maximum (IC50) of 1.09 μM.</p>

<p>Protein Kinase C (19-31) TFA is a serine-modified PKCa-derived inhibitor for testing PKC activity.</p>

<p>αvβ6-IN-1 (compound 28) is an effective orally active inhibitor of αvβ6 integrin (αvβ6integrin), with a pIC50 value of 8.1. This compound shows potential for research in idiopathic pulmonary fibrosis.</p>

<p>Compound 6h (Anticancer Agent 139) exhibits potent anticancer activity, engaging in a π-cationic interaction with Lys352 of Tubulin and demonstrating high</p>

<p>Aβ-IN-1 TFA inhibits and reverses different types of protein aggregation.</p>

<p>αvβ6-IN-2 (compound 20) is an effective orally active inhibitor of αvβ6 integrin (αvβ6integrin), with a pIC50 value of 7.8. It shows potential for use in research on idiopathic pulmonary fibrosis.</p>

<p>EMD527040 is a potent αvβ6 antagonist with antifibrotic effects, used in carcinoma and liver fibrosis research.</p>

<p>Compound 3l, a paclitaxel derivative known as Microtubule Stabilizing Agent-1, effectively enhances tubulin polymerization and demonstrates antitumor efficacy [</p>

<p>Anticanceragent 270 (Compound 8e) is a microtubule protein inhibitor with an IC50 of 1.02 μM against MCF-7 breast cancer cells. It exerts significant antiproliferative activity on breast cancer cells through a dual mechanism of inducing apoptosis and destabilizing microtubules. Anticanceragent 270 is useful for cancer research.</p>

<p>MT189 (Antiproliferative agent-14) inhibits tubulin polymerization (IC50 3.41 μM), arrests G2/M cell cycle, and is highly antiproliferative.</p>

<p>ML 2-23 is a potent BCR-ABL degrader operating as a PROTAC, exhibiting selective proteasome-dependent degradation of BCR-ABL within leukemia cells [1].</p>

<p>Zolbetuximab MMAE (IMAB362 MMAE) is a compound targeting Claudin 18.2 (CLDN18.2) with anti-cancer activity, used in the study of gastric and pancreatic cancers.</p>

<p>Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM.</p>

<p>BCR-ABL-IN-9 (Compound B1) is an inhibitor of BCR-ABL that achieves sustained suppression through the formation of stable covalent bonds with the ABL kinase. It effectively inhibits the activity of ABL kinase (IC50 = 1.2 nM) and possesses anticancer activity.</p>

<p>TNIR7-1A is a fused cycloheptatriene-BODIPY derivative that is optimized for near-infrared (NIR) imaging characteristics (Ex/Em = 600/774 nm in PBS) and exhibits high affinity and specificity for neurofibrillary tangles (NFT) in vitro. Additionally, TNIR7-1A can effectively penetrate the blood-brain barrier.</p>

<p>Bimosiamose has anti-inflammatory effects[1].</p>

<p>HA15-Biotin, a synthetic HA15-biotin conjugate, shows similar activity and may aid in proteomics.</p>

<p>ICAM-1988 is a LFA-1 antagonist.</p>

<p>GSK-3β Inhibitor21 (compound 44) is an ATP-competitive inhibitor of GSK-3β with an IC50 value of 6.06 µM, characterized by its ability to inhibit tau phosphorylation and prevent amyloid protein aggregation. This compound is utilized in the research of Alzheimer's disease.</p>

<p>Ganodermaones B is a renal fibrosis inhibitor. Ganodermaones B inhibits TGF-β1-induced collagen I and fibronectin expression .</p>

<p>Wnt pathway inhibitor 4 is a small molecule antimicrobial agent with antibacterial and antiproliferative activity against cancer cells.</p>

<p>Potent antagonist of the integrin αvβ3-vitronectin interaction (IC50 = 25.72 nM). Blocks proliferation and induces apoptosis in HUVECs; antiangiogenic.</p>

<p>Epothilone F, an active metabolite of Epothilone D with a hydroxymethyl on thiazole, disrupts cell division, shows promise over taxanes, and is water-soluble.</p>

<p>α2β1 Integrin Ligand Peptide TFA interacts with the integrin receptor on the cell membrane and enters the cell to mediate extracellular signaling.It is a</p>

<p>Asperosaponin V is a useful organic compound for research related to life sciences. The catalog number is T126228 and the CAS number is 120481-38-1.</p>

<p>TPR proteins including CHIP, TPR1, and hSGT affect luciferase refolding by DnaJ and hsc70.</p>

<p>Foxy-5 is a wnt5a peptide mimetic</p>

<p>OXi-4503, a prodrug of Combretastatin A-1, disrupts tubulin, inhibits Wnt/β-catenin and AKT, and has anti-tumor/vascular effects.</p>

<p>11H-Benzo[a]carbazole is a kinesin-like protein KIF11 inhibitor that can inhibit the viability of HeLa cells.</p>

<p>DSPE-PEG1000-iRGD is a PEG compound made from DSPE and the αv-integrin-targeting peptide (iRGD). The iRGD peptide initially binds to αv-integrins and undergoes proteolytic cleavage within tumors to produce CRGDK/R, which interacts with neuropilin-1, thereby facilitating tumor targeting and penetration. DSPE-PEG1000-iRGD is useful for drug delivery applications.</p>

<p>SNIPER(ABL)-058, a compound that links Imatinib (ABL inhibitor) with a derivative of LCL161 (IAP ligand) through a linker, effectively decreases BCR-ABL protein</p>

<p>3-Phenyltoxoflavin (Phenyltoxoflavin) is an inhibitor of HSP90 (Kd = 585 nM) with anti-cancer activity.</p>

<p>Maydispenoid B suppresses immune response, halts mouse spleen cell growth.</p>

<p>Betamethasone 17-benzoate is a representative steroid. It also can be used in the treatment of recurrent aphothous ulcers (RAU).</p>

<p>MS170, specific PROTAC AKT degrader, potent with DC 50 of 32 nM, binds AKT1/2/3 with Kd 1.3, 77, 6.5 nM respectively.</p>

<p>PDS-0330, a claudin-1 inhibitor, hinders CRC growth and metastasis with micromolar affinity and promising pharmacokinetics.</p>

<p>Phomopsin A is a cyclic hexapeptide mycotoxin isolated from the fungus Phomopsis leptostomiformis.</p>

<p>Dafsolimab (SPV-T3a), an IgG2a murine monoclonal antibody (anti-CD3), induces cell death by modulating and activating the CD3/T cell receptor complex and is</p>

<p>P8RI acetate mimics CD31, activates CDP8RI, and suppresses the immune response by restoring CD31 pathway.</p>

<p>Larazotide: octapeptide from V. cholerae, treats Coeliac disease by inhibiting paracellular permeability.</p>

<p>Bifidenone is an effective tubulin polymerization inhibitor.</p>

<p>HSP70-IN-3: Strong HSP70 blocker; IC50=1.1μM/1.9μM (ASZ001/C3H10T1/2); hinders Hedgehog signaling and cancer cell growth, lowers GLI1 levels.</p>

<p>Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a microtubule polymerization inhibitor prodrug mediated by Pd. Developed from colchicine-binding site inhibitors (CBSIs), it aims to reduce toxicity and enhance targeted release. Compared to the parent compound, its cytotoxicity is decreased by 68.3 times, but can be in situ restored in the presence of Pd resin. Mechanistic studies show it retains the same antitumor activity as CBSIs. In vivo tests demonstrate that, once activated by Pd resin, it significantly suppresses tumor growth (63.2% inhibition rate). Tubulin Polymerization-IN-1 prodrug is a promising candidate for cancer research.</p>

<p>Compound X10g (PROTAC Hsp90α degrader 1) is a selective agent targeting Hsp90α for degradation and is utilized in breast cancer research.</p>

<p>MK2-IN-5, a pseudosubstrate of Mk2 with an inhibition constant (K_i) of 8 μM, selectively targets the protein interaction domain of the MAPK pathway and</p>

<p>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</p>

<p>A unique collection of 1016 tyrosine kinase inhibitors for high throughput screening and high content screening for drug discovery in tyrosine kinase related</p>

<p>Sangivamycin (NSC-65346) inhibits PKC (Ki=10μM) and hinders growth in various human cancers.</p>

<p>Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.</p>

<p>Tubulin polymerization-IN-53 (compound 4b) serves as an inhibitor of β-tubulin polymerization and is capable of arresting the cell cycle at the G2/M stage.</p>

<p>AT7867 dihydrochloride inhibits Akt1/2/3 and p70S6K/PKA, with IC50s: 32/17/47 nM &amp; 85/20 nM, respectively, and hampers tumor growth.</p>

<p>Trifluralin (Treflan) is an agricultural herbicide with mild toxicity. Trifluralin is a novel pollutant that can interfere with mitochondrial respiration.</p>

<p>TTBK1-IN-1 (compound 31) is a potent and selective TTBK1 inhibitor with CNS penetration that inhibits tau phosphorylation , Alzheimer's disease.</p>

<p>Lixisenatide: Injectable GLP-1 agonist for T2DM, controls blood sugar.</p>

<p>NSC305787 hydrochloride ((Rac)-NSC305787 hydrochloride is a Cdc25 dual specificity phosphatase and EZR inhibitor with antitumor activity and inhibits Cdc25B2.</p>

<p>Miransertib hydrochloride is an orally active, selective, allosteric pan-Akt inhibitor that also demonstrates potent activity against Leishmania parasites.</p>

<p>DOTA-cyclo(RGDfK) is a and DOTA-like chelator peptide,the αvβ3 integrin receptor ,radionuclide coupled compounds RDCs cancer diagnostics and therapy.</p>

<p>Tonabersat (SB-220453) is a novel and orally available gap-junction modulator and CSD (Cortical spreading depression) inhibitor that,migraine and epilepsy.</p>

<p>Blinatumomab (AMG-10,MT-103) is a CD19/CD3 bispecific B-cell and T-cell binding antibody that in acute lymphoblastic leukemia and non-Hodgkin's lymphoma.</p>

<p>Anti-Mouse CD3 Antibody (17A2) is an IgG2b class antibody of murine origin targeting CD3 and can be used to study TCR signaling and antigen recognition.</p>

<p>MK-0429 is an orally active, selective, and nonpeptide antagonist of αvβ3 integrin (IC50: 80 nM).</p>

<p>xStAx-VHLL TFA is a β-catenin degrader formed by coupling xStAx to VHL ligand, with anti-cancer activity and inhibition of Wnt signaling.</p>

<p>Avanbulin hinders tubulin polymerization, has unique antitumor properties, and is effective against various human tumors at low concentrations.</p>

<p>Danegaptide (GAP-134) is a potent, second-gen, oral gap junction modifier; a small modified dipeptide.</p>