Angiogenèse

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.

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

DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP[1].

AT-533 inhibits Hsp90, HSV, hinders HIF-1α/VEGF/VEGFR-2, Erk1/2, FAK, Akt/mTOR/p70S6K, and blocks tumor growth, angiogenesis, and HUVEC activities.

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

Glaziovine is an agent of anti-ulcerogenic natural alkaloid.

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

EGFR-IN-140 (Compound 31) is an inhibitor of EGFR, effectively targeting both wild-type EGFR and the EGFRL858R/T790M/C797S mutant, with Ki values of 0.95 nM and 2.1 nM, respectively. Additionally, it inhibits EGFRdel19/T790M/C797S in Ba/F3 cells with an IC50 of 56.9 nM and demonstrates antitumor activity in mouse models.

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

Potent PROTAC degrader for FLT3/CDK9, induces apoptosis, and shows promise for FLT3-ITD mutated AML research.

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.

DBt-10 is a potent Bruton's tyrosine kinase (BTK) degrader [1].

ALK/ROS1-IN-3 (compound C01) is a dual inhibitor targeting ROS1 and ALK, with IC50 values of 42.3 nM for ROS1G2032R and 49.1 nM for ALKG1202R.

TLT8 is a ByeTAC protein degrader that targets BTK. It induces BTK degradation by non-covalently binding to Rpn-13 and BTK. TLT8 is applicable in research on chronic lymphocytic leukemia.

Wu-5 is a potent USP10 inhibitor that inhibits FLT3 and AMPK pathways, promoting the breakdown of FLT3-ITD and inducing apoptosis.

PROTAC EGFR degrader 5 effectively breaks down EGFR Del19 in HCC827 cells at 34.8 nM, inducing apoptosis and G1 arrest.

Zeteletinib hemiadipate (BOS-172738; DS-5010) is an oral RET kinase blocker with nanomolar potency and strong anti-tumor properties.

IMS2186: antichoroidal neovascularization reagent, arrests G2/M cancer phase, anti-proliferative, reduces eye leakage, non-toxic.

BCPyr is a new candidate BTK degrader ( DC 50 = 800 nM).

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.

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

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.

FAK PROTAC B5: a degrader with 14.9 nM IC50, strong degradation, anti-growth, good plasma stability, and fair permeability.

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.

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.

PROTAC EGFR degrader 4 targets mutant EGFR, degrades del19 and L858R/T790M (DC50: 0.51, 126 nM), and inhibits HCC827, H1975 cell growth (IC50: 0.83, 203.1 nM).

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].

PROTAC TYK2 Agent1 selectively degrades TYK2, with a 14 nM DC50, for autoimmune research.

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

AG1478 HCl is an epidermal growth factor receptor protein inhibitor.

SA-VA, an intracellular self-assembled PROTAC featuring azide and alkyne groups, selectively degrades VEGFR-2 and EphB4 proteins within U87 cells.

SNIPER(ABL)-015, a compound that conjugates GNF5 (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels with a DC50 of 5

Inhibits Lyn kinase, blocks IL-5 receptor, prevents eosinophil differentiation and reduces asthma-related inflammation in mice.

Lyso-Monosialoganglioside GM3 (Lyso-GM3) is an analog of Ganglioside GM3 with antitumor properties. It inhibits the increase in EGFR kinase activity induced by EGF in A431 epithelial cancer cells.

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

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.

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.

Ibrutinib-biotin probe links Ibrutinib to biotin, with IC50 0.755-1.02 nM for BTK (patent WO2014059368A1).

Adenosine receptor modulator 1 acts as an inducer of collagen VII (C7). It enhances the expression of COL7A1 mRNA in donor-derived keratinocytes and, in synergy with Gentamicin, increases the overall levels of C7.

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

EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively.

BIIB091 is a highly selective, reversible BTK inhibitor for treating autoimmune diseases.

PROTACFLT3/CDKs degrader-1 (Compound C3) is an agent that degrades cyclin-dependent kinase (CDK2 with a DC50 of 18.73 nM) and FMS-like tyrosine kinase 3 (FLT3). It induces differentiation in HL-60 cells, achieving a 72.77% differentiation rate at 6.25 nM, and inhibits proliferation of acute myeloid leukemia (AML) cells, with an IC50 ranging from 2.9 to 37 nM. PROTACFLT3/CDKs degrader-1 demonstrates potential for improving the treatment of AML.

SNIPER(ABL)-047, a compound that links HG-7-85-01 (an ABL inhibitor) to MV-1 (an IAP ligand) via a linker, effectively decreases the BCR-ABL protein levels,

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.