Angiogenesi

<p>JH-XI-10-02 selectively degrades CDK8 (IC50: 159 nM) through proteasome, sparing CDK8 mRNA and CDK19.</p>

Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ).

<p>TYD-68 is a potent and selective CRBN-recruiting TYK2 PROTAC degrader, with a DC50 value of 0.42 nM. This compound effectively inhibits IL-12 and IFN-α-induced phosphorylation of STAT4 and STAT1, thereby blocking TYK2-dependent signaling pathways. TYD-68 is applicable in psoriasis research.</p>

GSK143: Oral SYK inhibitor, pIC50=7.5, curbs pErk, anti-inflammatory, hinders immune cells in mice.

<p>Abicipar pegol is an anti-VEGF DARPin for ocular diseases, reducing retinal thickness and leakage.</p>

FGFR2 degrader1 (compound 28E) is a selective PROTACS degrader of FGFR2, with a DC50 of 0.645 nM. FGFR2 plays a significant role in cancer research.

<p>HER2-IN-20 (compound 32) is a potent and selective inhibitor of HER2WT and HER2YVMA, with IC50 values of 49 and 42 nM, respectively. It holds potential for research in non-small cell lung cancer (NSCLC).</p>

BV02 blocks 14-3-3 interactions, useful in chronic myeloid leukemia research, targets T315I mutant and wild-type Bcr-Abl cells.

<p>Potent, selective oral PROTAC BTK Degrader-1; IC50: 34.51 nM (WT), 64.56 nM (BTK-481S); reduces BTK protein, inhibits tumors.</p>

<p>MHES0488A is a selective humanized antibody targeting HER2, with a KD value of 0.8 nM. It constitutes the antibody portion of DHES0815A. Upon cellular internalization, MHES0488A is transported to lysosomes, releasing PBD-monoamide into the nucleus, where it alkylates DNA, inducing DNA damage and apoptosis. It shows potential for research in cancers such as HER2-positive breast cancer and gastric cancer.</p>

Syk-IN-4: potent, selective SYK inhibitor, orally bioavailable, IC50=0.31 nM, targets autoimmunity, cancers.

EGFR-IN-42 (17b) is a potent EGFR inhibitor with nanomolar efficacy, merging tamoxifen/endoxifen and gefitinib, exhibiting enhanced anti-cancer action.

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

AD57, a polypharmacological agent, blocks RET kinase (IC50: 2 nM), disrupts related kinases, and hinders cancerous activities like invasion and proliferation.

SJ988497: PROTAC JAK2 degrader, inhibits CRLF2r cell growth, degrades GSPT1, combines Ruxolitinib, linker, Pomalidomide; researched for ALL.

Multi-kinase-IN-5 (compound 15c) is a multi-kinase inhibitory agent that shows significant inhibition against a range of protein kinases including RET, KIT,

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

<p>BMS-599626 2HCL (AC480 2HCl) is a BMS-599626 derivative.</p>

SJF620 hydrochloride is a PROTAC that utilizes a lenalidomide analog to recruit CRBN and ligands to target Btk, exhibiting a DC50 of 7.9 nM [1].

Bevasiranib is a siRNA targeting VEGF production, key in choroidal neo-vascularization and wet AMD.

M4K2234 (26b) inhibits ALK2/ALK5 (IC50: 5/2144 nM), used as a probe for ALK1/2 kinases in cancer research.

SPP-037 is an orally active selective inhibitor of ST6GAL1, with an IC50 of 3.59 μM. It exhibits anti-migration activity against MDA-MB-231 cells by inhibiting integrin α2,6-sialylation and the integrin-FAK-paxillin pathway. In MDA-MB-231 xenograft mouse models, SPP-037 demonstrates antitumor properties. This compound is applicable in breast cancer research.

PTD10, a highly potent PROTAC BTK degrader, exhibits a DC50 of 0.5 nM and a KD of 2.28 nM.

(R)-3-Hydroxy Midostaurin: potent kinase inhibitor, major midostaurin metabolite via CYP3A4, potential AML treatment.

<p>FW-1 is a type I inhibitor of FLT3, with an IC50 of approximately 1 μM. It exhibits cytotoxic effects in FLT3-mutant AML cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis in MV4-11 and MOLM-13 cells.</p>

SNIPER(ABL)-019, a compound that links Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, exhibiting a

<p>EGFR-IN-22: potent for EGFR (IC50: 4.91 nM) &amp; L858R/T790M/C797S mutation (IC50: 0.54 nM).</p>

JBJ-09-063 TFA, an EGFR inhibitor selective for EGFR mutations, IC50s: 0.147-0.396 nM, blocks EGFR/Akt/ERK signaling, for EGFR-mutant lung cancer research.

PROTAC ALK degrader-3 (4B) is an orally active PROTAC-based ALK degrader, efficiently inducing sustained degradation of ALK fusion protein and significant inhibition of downstream pathways in Karpas 299 cells with an IC50 of 119.33 nM. This compound exhibits antitumor activity.

<p>EGFRT790M/L858R-IN-2: selective inhibitor, IC50: 3.5 nM (mutant), 1290 nM (WT); reduces p-EGFR/AKT/ERK1/2, triggers apoptosis, G1 arrest, anti-cancer.</p>

SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker.

NRX-0492: orally active BTK degrader, induces ubiquitylation/proteasomal breakdown, potent with DC50 ≤0.2 nM, DC90 ≤0.5 nM, disrupts BCR signaling.

EGFR/CDK2-IN-2 (compound 6a) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 19.6 nM and 87.9 nM, respectively.

<p>ALK/ROS1-IN-5 (compound X4) is a selective inhibitor of ALK and ROS1 kinases, with IC50 values of 0.512 μM for ALK and 0.766 μM for ROS1. It inhibits H2228 cells with an IC50 of 0.034 μM and induces apoptosis in cancer cells in a dose-dependent manner. Additionally, ALK/ROS1-IN-5 effectively suppresses the expression of p-ALK and p-ERK in cancer cells.</p>

<p>A unique collection of 1353 proangiogenic and antiangiogenic compounds for new targets identification, research in mechanisms of angiogenesis, and high</p>

MS9449 is a powerful EGFR PROTAC; Kd: 17 nM (WT), 10 nM (L858R); targets mutant EGFRs via UPS and autophagy; hinders NSCLC cell growth.

Compound 5K (Multi-target kinase inhibitor 2) is a multi-targeted kinase inhibitor demonstrating activity against EGFR, Her2, VEGFR2, and CDK2 with IC50 values

<p>VSLRGDTRG acetate is a synthetic peptide of the RGD motif from cadherin17 (CDH17), capable of binding to α2β1 integrin and activating its signaling pathways. It facilitates the high-affinity conformational change of β1 integrin via the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby promoting tumor proliferation and metastasis. VSLRGDTRG acetate is applicable in research on cancers expressing CDH17, such as colon and pancreatic cancers.</p>

<p>KIT/PDGFRA-IN-1 (compound 19) is an inhibitor targeting the stem cell growth factor receptor (KIT) and platelet-derived growth factor receptor alpha (PDGFRA). Its IC50 values are 2.3 µM for KIT-wt, 12 µM for KIT-D816H, 492 µM for KIT-T670I, 0.8 µM for PDGFRA-wt, 99.9 µM for PDGFRA-D842V, 42.3 µM for PDGFRA-T674I, and 4.3 µM for PDGFRA-G680R. The GR50 values for GIST-T1, T1-a-D842V, and GIST-48B cell lines (gastrointestinal stromal tumor cell lines with PDGFR and KIT mutations) are 12 nM, 8900 nM, and ≥10,000 nM, respectively.</p>

Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.

FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor properties. It selectively targets cancer cells with FLT3 internal tandem duplication (ITD) mutations, demonstrating IC50 values of 85, 290, 130, 65, and 220 nM against BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively. These lines include acute myeloid leukemia (AML) cells harboring FLT3-ITD mutations such as MV4-11 and MOLM-13/14. The compound also reduces phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells, leading to cell cycle arrest and apoptosis. With an oral bioavailability of 19.2% in SD rats, FLT3-IN-28 extends survival in a dose-dependent manner in MOLM-13 xenografted NSG mouse models. It holds promise for research in FLT3-ITD-related cancer studies.

<p>SJF 1521 is an EGFR degrader belonging to the PROTAC class that selectively degrades EGFR while preserving HER2.</p>

<p>Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.</p>

AG-825（Tyrphostin C15） is a selective and competitive ErbB2 inhibitor that inhibits tyrosine phosphorylation with an IC50 value of 0.35 μM.AG-825 (Tyrphostin

<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>

VSLRGDTRG is a synthetic peptide derived from the RGD motif in cadherin17 (CDH17) that binds to the α2β1 integrin, activating its signaling pathways. By promoting high-affinity conformational changes in β1 integrins through the RGD motif, VSLRGDTRG enhances cell adhesion and the phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. This peptide is useful for research on cancers expressing CDH17, such as colorectal and pancreatic cancer.

<p>HIF-1 inhibitor-4 (HIF-1 inhibitor-4) is a HIF-1 inhibitor with IC50 of 560 nM.</p>

SNIPER(ABL)-044, a compound that links HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, achieving a

Emavusertib (CA-4948) hydrochloride, a selective and potent IRAK4/FLT3 inhibitor, is designed for oral administration. It achieves an IC 50 of 57 nM against IRAK4 in a FRET kinase assay and demonstrates anti-tumor activity [1] [2] [3].

<p>EGFR-IN-110 (Compound 6) is a covalent inhibitor of EGFR, demonstrating pIC50 values of 9.2 for the EGFR enzyme and 8.7 for EGFR cells. It exhibits strong efficacy in targeting EGFR and maintains good kinase selectivity.</p>

<p>FDU73 is a potent and selective BTK PROTAC degrader with a DC50 of 2.9 nM in JeKo-1 cells. It inhibits tumor cell proliferation and exhibits antitumor activity.</p>

Mersalyl is an organic mercurial diuretic.

<p>Vulinacimab (HLX-06) is a mAb targeting VEGFR-2, used in cancer research, vital for tumor angiogenesis and endothelial cell functions.</p>

<p>AMX-818 is a conditionally activated, masked T cell engager (TCE) that targets HER2. It demonstrates potent T cell cytotoxicity against HER2-positive tumor cell lines and can induce tumor regression in vivo. AMX-818 holds promise for research into HER2-positive solid tumors.</p>

<p>IOX2-NH2-Methyl is a modified form of IOX2. IOX2 is a specific inhibitor of PHD2 (prolyl-hydroxylase-2), capable of upregulating HIF-1α expression and suppressing ROS production. IOX2-NH2-Methyl is employed in investigations of platelet and thrombus formation.</p>

AG1478 HCl is an epidermal growth factor receptor protein inhibitor.

<p>A unique collection of 1336 HIF-1 related small chemicals can be used for drug discovery in ischemic disease and cancer and related mechanism studies；</p>

<p>JAK3-IN-14 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively.</p>

<p>Sorafenib D4 is deuterium-labeled Sorafenib, a multi-kinase inhibitor (Raf-1, B-Raf, VEGFR-3) with IC50s: 6, 20, 22 nM.</p>

FLT3-IN-24 (compound 24) is a potent and selective inhibitor of FLT3 kinase, with an IC50 of 7.94 nM. It also exhibits anti-proliferative effects on cells.

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

<p>CEP-5214: Powerful pan VEGF-R tyrosine kinase inhibitor; IC50: 16nM (R1), 8nM (R2), 4nM (R3); effective in cells.</p>

<p>EGFR/DHFR-IN-1 (Compound 10e) is a dual inhibitor of EGFR and DHFR, with IC50 values of 0.151 µM and 0.541 µM, respectively. It induces cell cycle arrest in the G0-G1 and S phases.</p>

<p>EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFRWT and 0.0438 μM for EGFRL858R/T790M. It exhibits antiproliferative activity, effectively inhibiting the proliferation of H1975 cells and inducing apoptosis (apoptosis). EGFR-IN-107 is applicable in cancer research.</p>

<p>MPT0B390 is an inhibitor of HDAC and a TIMP3 inducer inhibiting tumor growth, metastasis, and angiogenesis.</p>

<p>HDS 029 has a wide range of applications in life science related research.</p>

Simotinib hydrochloride: selective oral EGFR inhibitor, IC50 19.9 nM, potent anticancer agent.

Phosphopeptide; binds to the src SH2 domain.

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.

<p>PROTAC BTK Degrader-6 (Compound 15), with a DC50 of 3.18 nM, exhibits anti-inflammatory properties by inhibiting NF-κB activation and suppressing the expression</p>

SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of

<p>EGFR-IN-95 is a derivative of 2,4-diaminonicotinamide. It effectively inhibits the activity of EGFRdel19/T790M/C797S and L858R/T790M/C797S.</p>

JAK 3 inhibitor IV (ZM 39923 hydrochloride) is a JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to

VnP-16 enhances bone formation by stimulating the differentiation and activity of osteoblasts via direct β1 integrin engagement, which subsequently activates

DB1113 is a bifunctional kinase degrader, targeting ABL1, ABL2, CDK4, MAPKs, and more for disease research.

<p>Syk signaling is key in lupus. Syk inhibitors reduce inflammation and sepsis severity in FcgRIIb-/- mice, lowering cytokines and organ damage.</p>

HAT-SIL-TG-1&AT: a hypoxia-activated JAK inhibitor that curbs HEL cell growth & STAT3/5 phosphorylation in tumors.

FLT3-IN-22 (compound 22f) is a potent inhibitor of FLT3, demonstrating IC50 values of 0.941 nM for FLT3 and 0.199 nM for the FLT3/D835Y mutant.

MS9427 TFA: PROTAC EGFR degrader, Kd 7.1 nM (WT), 4.3 nM (L858R), targets mutant EGFR, inhibits NSCLC cell growth, for cancer research.

SNIPER(ABL)-033, a compound that conjugates HG-7-85-01 (ABL inhibitor) to a LCL161 derivative (IAP ligand) via a linker, effectively reduces BCR-ABL protein

<p>SIAIS164018 hydrochloride is a PROTAC-based degrader targeting ALK and EGFR, exhibiting IC50 values of 2.5 nM for ALK and 6.6 nM for ALK G1202R.</p>

<p>PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) (IC50 of 6.5 nM).</p>

HSK205 is a dual FLT3 and haspin inhibitor, exhibiting potent antitumor activity [1], with an IC50 of 0.187 nM for FLT3.

ALK-IN-9 effectively inhibits cell growth with IC50 <0.2 nM for Ba/F3-EML4-ALK, KM12, KG-1.

<p>PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production</p>

QL-X-138 HCl is a BTK/MNK dual kinase inhibitor with anticancer activity and anti-dengue virus 2 activity that inhibits BTK, MNK1, and MNK2 kinases.

PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual inhibitor targeting PRMT5 and EGFR, with IC50 values of 15.47 μM and 19.31 μM, respectively. It demonstrates antiproliferative activity against the A549, MCF7, HeLa, and MDA-MB-231 cell lines. This compound also exhibits favorable pharmacokinetic (PK) and pharmacodynamic (PD) properties in vivo and significantly inhibits the growth of MCF7 orthotopic xenograft tumors.

<p>MR44397 is a ligand for WD40 repeat (WDR) 5 and is applicable in cancer research.</p>

<p>BTK-IN-5 is a covalent inhibitor of Bruton's tyrosine kinase (BTK) designed for the treatment of medical conditions including cardiovascular diseases,</p>

FAK-IN-14 is a FAK inhibitor that induces apoptosis and cell cycle arrest. FAK-IN-14 has a more significant inhibitory effect on FAK, FGFR1 and Pyk2.

<p>WDR5ligand 2 is a ligand for WDR5 and can be utilized in the synthesis of PROTAC WDR5degrader 1.</p>

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.

<p>PROTACEGFRdegrader 9 (Compound C6) is an orally active, CRBN-based PROTAC EGFR degrader. It has a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFRL858R/T790M/C797S. PROTACEGFRdegrader 9 demonstrates effective degradation activity against various EGFR mutants while not affecting EGFRWT.</p>

CS-VIP 8 TFA is a selective allosteric inhibitor of the WDR5 protein (Ki= 0.008 μM). It induces a conformational change in the MLL1 complex, leading to the dissociation of MLL1 from the complex, thereby inhibiting the MLL1 histone methyltransferase activity and modulating HOX gene expression. CS-VIP 8 TFA shows potential for research in hematological disorders such as leukemia.

hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide with potential as a dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2.

PF15 TFA, a PROTAC targeting FLT3 kinase and CRBN, exhibits selective degradation of FLT3-ITD with a DC50 of 76.7 nM.

<p>DSPE-PEG1000-GE11 is a PEG compound made up of DSPE and an EGFR-targeting peptide (GE11). GE11 is applicable for cancer cells overexpressing EGFR. DSPE-PEG1000-GE11 serves a role in drug delivery.</p>

<p>TYK2activator-1 (16b) is a TYK2 activator with an EC50 value of 1.78 μM. It inhibits JAK2 and JAK3 with IC50 values of 6.8 μM and 6.3 μM, respectively.</p>

VEGFR-2-IN-64 (Compound 28) is an inhibitor of VEGFR2 with an IC50 of 27.8 nM. It suppresses the proliferation of cancer cells A549, T-47D, and Caco-2, exhibits anti-migration and anti-colony formation activities in T-47D cells, and induces apoptosis in T-47D cells.

VEGFR-2-IN-66 (Compound 6) is an orally active VEGFR-2 inhibitor with an IC50 of 0.509 µM and an IC50 value of 7.48 μM for inhibiting MCF-7 cell proliferation. Its anticancer activity is exerted through cell cycle arrest, induction of apoptosis (Apoptosis), and modulation of gene expression, making it suitable for breast cancer research.