UT-59 is a specific inhibitor of cholesterol-sensing membrane protein Scap, binds to Scap's cholesterol-binding site, blocks SREBP activation and inhibits lipid synthesis.

UTBinh-14 is a potent, highly selective inhibitor for urea transporter UT-B with IC50 of 11 nM, with over a thousand-fold selectivity over UT-A.

VJDT (TREM1 inhibitor) is a novel small molecule inhibitor of triggering receptor expressed on myeloid cell 1 (TREM1), effectively blocks TREM1 signaling.

WX-02-37 is a selective, allosteric and covalent inhibitor of sterile alpha toll/interleukin receptor motif containing-1 (SARM1) with IC50 of 1.5 uM, site-specifically and stereoselectively modify cysteine-311 (C311) in the noncatalytic, autoregulatory ar

XEN 602 (XEN602) is a potent, specific divalent metal transporter 1 (DMT1) inhibitor that inhibits Mn incorporation in HEK293 cells with IC50 of 0.3 nM.

A substrate for chromogenic assay of neuraminidase activity in bacterial expression systems..

XST-20 is a small molecule selectively targeting FOXM1 DNA-binding domain (DBD) with SPR Kd of 20 uM, effectively suppresses FOXM1 transcriptional activities and inhibits ovarian cancer cell proliferation.

YB-537 (YB537) is a potent, highly specific quinone reductase 2 (QR2) inhibitor with IC50 of 3 nM, shows no activity against QR1 (IC50>10 uM).

YE6144 (YE 6144) is a specific small molecule inhibitor of transcription factor IFN regulatory factor 5 (IRF5), selectively suppresses IRF5 activity through inhibition of IRF5 phosphorylation.

YL-365 (YL365) is a highly potent, selective and competitive antagonist of GPR34.

Z839878730 (KK-LC-1 inhibitor Z8) is a small moelcuel compound targeting KK-LC-1, which is significantly highly expressed in triple-negative breast cancer tissues than in normal breast tissues.

ZHAWOC8697 is a small molecule dual inhibitor of sentrin-specific protease SENP1 and SENP2 with IC50 of 8.6 and 2.3 uM, respectively, a valuable tool for the study of SUMOylation processes.

ZINC13407541 is a small molecule antagonist for FGF23, inhibits FGF-23 signaling with IC50 of 0.45 uM.

ZINC16991592 is a selective MRGPRX2 antagonist with Ki of 189 nM.

ZYF0033 (ZYF 0033) is potent, selective, small-molecule inhibitor of HPK1 with IC50 of <10 nM based on the phosphorylation inhibition of MBP protein.

ψTnI (Peptide DWRKNIDA) is a selective, high-affinity, eight amino acid peptide inhibitor of cardiac troponin I (cTnI), directly binds to δPKC with high affinity (Kd=5 nM) and inhibits cTnI/δPKC interaction.

7030B-C5 is an effective small-molecule PCSK9 inhibitor with IC50 of 1.61 uM (PCSK9 transcription) in HepG2 cells, with no apparent effect on cell growth and survival.

NYX-1492 is a small molecule PCSK9 inhibitor, blocks PCSK9 binding with the LDLR, attenuates inflammation in vascular cells and tissue-engineered blood vessels (TEBVs).

NYX-PCSK9i is an orally bioavailable small-molecule inhibitor of PCSK9, inhibits PCSK9-LDLR interaction with IC50 of 323 nM in in vitro biochemical binding assays.

BPN-15477 (BPN15477) is a potent splicing modulator compound that restores correct splicing of ELP1 exon 20, increases full-length ELP1 mRNA by increasing exon 20 inclusion with EC50 of 1.9 uM in luciferase splicing assays.

CD33 splicing modulator 1 is a small-molecule CD33 pre-mRNA splicing modulator with EC50 of 7.8 uM, enhances the exclusion of CD33 exon 2, reduces full-length V-domain containing CD33 protein.

HTT splicing modulator 27 is a potent, orally bioavailable, and brain-penetrant small-molecule HTT pre-mRNA splicing modulator with mHTT protein EC50 of 66 nM.

Rebecsinib (17S-FD-895) is a selective small-molecule inhibitor of splicing-mediated ADAR1 activation, prevents leukemia stem cell generation.

Thailanstatin C (TST-C) is a potent antiproliferative natural product, a pre-mRNA splicing inhibitor and antiproliferative agent..

SRI-42127 is a small molecule, BBB-permeable inhibitor of the RNA regulator HuR, inhibits HuR dimerization with IC50 of 1.2 uM in cell-based assays, prevents HuR oligomerization.

STK018404 is a small molecule inhibitor of RNA-binding protein human antigen R (HuR), decreases the binding of HuR to its target RNA motif.

AA132 (AA-132) is a small molecule activator of UPR signaling, covalently modifies a subset of ER protein disulfide isomerases (PDIs), activates global UPR signaling through a mechanism analogous to that of AA147.

AG-946 (AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively.

HA344 (HA 344) is a dual covalent inhibitor of pyruvate kinase M2 (PKM2) and inosine monophosphate dehydrogenase (IMPDH), efficiently inhibits cutaneous metastatic melanoma (CMM).

TAS0612 (TAS-0612) is an orally bioavailable multikinase inhibitor of AKT, p70S6K, and p90RSK, inhibits Y-box-binding protein (YBX1) phosphorylation.

TCMDC-136364 (AKT Kinase Inhibitor) is an Akt kinase inhibitor, selectively inhibits Akt in proliferating cells expressing Trop-2, also potently inhibits P. falciparum multidrug resistant strain Dd2.

BI-9774 (BI 9774) is a potent pan-AMPK activator with EC50 of 64 nM in an ADP-Glo kinase assay with human AMPK (α1β1γ1) and EC50 of 8 nM in a cellular GLUT4 translocation assay.

KI-301670 is a novel potent, specific NUAK1 inhibitor, disturbs NUAK1 signaling by targeting its ATP binding site, effectively inhibits the PI3K/AKT pathway in pancreatic cancer cells.

MSG011 is a potent, pan AMPK isoform activator with EC50 of 140.4 nM, 248.9 nM, 553.4 nM, and 472.9 nM for α1β1γ1, α1β2γ1, α2β1γ1, and α2β2γ1, respectively.

PXL770 is a novel orally bioavailable, small-molecule direct AMPK activator with EC50 of 16.2, 42.1 and 64 nM for α1β1γ1, α1β1γ2 and α1β1γ3, directly increases AMPK activity by both allosteric activation and protection from dephosphorylation.

PXL770 is a novel orally bioavailable, small-molecule direct AMPK activator with EC50 of 16.2, 42.1 and 64 nM for α1β1γ1, α1β1γ2 and α1β1γ3, directly increases AMPK activity by both allosteric activation and protection from dephosphorylation.

RX-375 (RX375) is an indirect small-molecule activator of AMPK by directly binds to Prohibitins (PHB1 and PHB2), induces dissociation of AMPK-PHBs complex.

ZLN-024 hydrochloride is a potent, allosteric AMPK activator that has no effect on mitochondrial function or the ADP/ATP ratio, directly activate recombinant AMPK α1β1γ1 and its homologue α2β1γ1 with EC50 of 0.42 uM and 0.95 uM, respectively.

NV-5297 (NV5297) is a novel small molecule mTORC1 pathway activator, modulates the Sestrin2-Gator2 interaction and activates the mTORC1 pathway in vitro and in vivo.

CU05-1189 is a non-peptide, allosteric inhibitor of the pleckstrin homology (PH) domain of PDK1, specifically inhibits Akt signaling pathway.

cyclo-CRVLIR is a cyclic peptide that binds selectively to p110α RAS binding domain (p110α-RBD) with ITC Kd of 3 uM, blocks p110α/RAS interaction in vitro and KRAS cancer cell lines.

HM5023507 is a potemt, selective, orally active dual PI3Kδ/γ inhibitor with IC50 of 4 nM and 5 nM for p110γ and p110δ, respectively.

I-229 is a potent and selective inhibitor of Vps34.

LL-00071210 is a potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 values of 24.6 nM and 9.4 nM in biochemical and cellular assays, respectively.

LL-00084282 is a potent, selective and efficacious dual PI3Kδγ inhibitor with IC50 of 16.26 and 17.45 nM for PI3Kδ and PI3Kγ, respectively.

LP-182 (LP182) is a potent, selective and orally bioavailable multi-functional kinase inhibitor, specifically targets PI3K and MAPK signaling pathways.

PF-06862309 (PF-06843195 phosphate ester prodrug) is the in vivo-active, phosphate ester prodrug of PF-06843195, a potent selective PI3Kα inhibitor with Kd of <18 pM.

PITCOIN2 (LU-06-006) is a potent selective PI3KC2α inhibitor with IC50 of 126 nM, has selectivity against PI3KC2γ but shows micromolar activity on PI3KC2β.

PITCOIN3 is a potent, highly selective, cell-permeable inhibitor of PI3KC2α catalytic activity with IC50 of 126 nM.

TGX286 is a potent, selective p110β inhibitor with IC50 of 7, 17 and 13 nM for p110β WT, p110β D862Q, and p110β E858H, respectively, >100-fold selectivity over p110α.

GSK-3923868 (PI4KB inhibitor 30) is a potent, selective, slow-dissociating PI4KB (PI4kIII-beta) inhibitor with pKi of 9.8, >1000-fold selectivity over PI4KA, inhibits HRV viral replication in COPD BECs.

HZX-02-059 is a PIKfyve and tubulin dual-target inhibitor with high affinity for PIKfyve (Kd=10.4 nM), HZX-02-059 is a potent methuosis inducer, shows both in vitro and in vivo anti-tumor activity against TNBC.

BAY-728 (NAY728) is a less potent enantiomer and negative control compound of BAY-805.

BK50118-C is a potent small molecule inhibitor of ubiquitin-specific protease-13 (USP13) with IC50 of 0.42 nM.

BML-260 (BML260) is a potent inhibitor of dual-specific phosphatase JSP-1 (JNK Stimulatory Phosphatase-1, DUSP22) and stimulator of uncoupling protein 1 (UCP-1) expression in adipocytes.

C598-0556 is a selective, small molecule inhibitor of USP10, inhibits USP10 comparably to HBX19818 (IC50=10 uM), with no inhibition against USP7 (IC50>100 uM).

C673-0105 is a selective, small molecule inhibitor of USP10, inhibits USP10 comparably to HBX19818 (IC50=10 uM), with no inhibition against USP7 (IC50>100 uM.

CAS-12290-201 is a potent and selective inhibitor of deubiquitinating enzyme (DUB) VCPIP1 with IC50 of 70 nM, covalently and specificly targets the catalytic cysteine of VCPIP1 with little to no activity toward other cellular DUBs.

DC-U4106 is a potent, selective small molecule inhibitor of Ubiquitin-specific protease 8 (USP8) with binding KD value of 4.7 uM, DC-U4106 is selective over USP2 and USP7.

FT206 (FT-206, FT3951206, CRT0511973) is a potent, selectivel inhibitor of USP28 with a remarkable USP28/25 selectivity.

FT385 (FT3967385) is a potent, selective USP30 inhibitor with biochemical IC50 of 1.5 nM.

GK13S is a highly potent, specific and covalent inhibitor of deubiquitinase UCHL1 with IC50 of 87 nM, displays exquisite specificity for UCHL1 over the other UCH family members (IC50>10 uM).

HY041004 is the first small molecule inhibitor of deubiquitinase Josephin Domain-containing protein 2 (JOSD2) with IC50 of 0.26 uM for JOSD2 catalytic activity inhibition.

I-138 (I 138) is a potent, specific small molecule USP1-UAF1 inhibitor with IC50 of 4.1 nM, binds to USP1-UAF1 at an allosteric pocket synergistically with ubiquitin.

IMP-2373 is a highly targeted cyanopyrrolidine (CNPy) probe for pan-DUB to monitor DUB activity in physiologically relevant live cells.

IU1-206 is a IU1 derivative with more potent activity against USP14, 10-fold more potent than IU1 and is comparable to the IU1-47.

IU2-6 is a small molecule USP14 inhibitor, shows 74% inhibition at 8 uM.

LN5P45 is a selective, covalent, irreversible inhibitor of ubiquitin thioesterase OTUB2 with IC50 of 2.3 uM, strongly induces monoubiquitination of OTUB2 on Lys31.

MS102 is a small molecule, orally available USP2 inhibitor with IC50 of 5.46 uM, induces transient degradation of ACE2 protein and inhibits ACE2-dependent coronavirus infection.

MTX115325 is a potent, selective, brain-penetrant USP30 inhibitor with IC50 of 12 nM in biochemical fluorescence polarization assays.

NCI677397 is a specific small molecule inhibitor of USP24, inhibits chemotherapy-induced drug resistance in vitro and in vivo.

OTUDin3 (OTUD3 inhibitor) is a specific, small molecule inhibitor of deubiquitylase OTUD3, binds to OTUD3 (KD=0.32 uM) and inhibits the deubiquitinating activity of OTUD3 by interfering with Ub binding to OTUD3.

SB1-F-70 is a potent, selective inhibitor of the deubiquitinase (DUB) JOSD1/USP30/UCHL1 with IC50 of 324/400/400 nM, respectively.

TG2-179-1 is a potent, selective and covalently inhibitor of deubiquitinase (DUB) BRCA1-associated protein-1 (BAP1), covalently binds to the active site of BAP1 (Cys91), exhibits potent cytotoxic activity against colon cancer cells.

USP7-797 is a novel potent selective inhibitor of USP7 with IC50 of 0.44 nM.

XL-9872-106C (XL-106C) is a potent, selective inhibitor of the deubiquitinase (DUB) JOSD1/USP30/UCHL1 with IC50 of 134/390/166 nM, respectively.

YCH2823 is a potent, selective USP7 inhibitor with IC50 of 49.6 nM, ITC Kd of 117 nM.

AAA-237 (AAA237) is a small molecule Skp2 E3 ligase inhibitor, binds to Skp2 protein (KD=28.77 uM) and inhibits the degradation of Skp2 substrates, inhibits the proliferation of the NSCLC cells.

BC18630 (BC 18630) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 39 nM in cell-based assays.

BC18630 free base (BC 18630) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 39 nM in cell-based assays.

BC18813 (BC 18813) is a small molecule inhibitor of the E3 ubiquitin ligase subunit DCAF7, potently inhibits SARS-CoV-2 infection with IC50 of 48 nM in cell-based assays.

NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research.

MN551 is a Cys111-specific, covalent ligand targeting the E3 ligase SOCS2 with ITC Ki value of 2.2 uM, blocks recruitment of cellular SOCS2 protein to its native substrate.

MN714 is a cell-premeable prodrug of MN551 containing a pivaloyloxymethyl (POM) and covalent inhibitor of E3 ligase suppressor of cytokine signaling 2 (SOCS2).

Skp2-2 is a small molecule inhibitor of Skp2-Cks1 interaction with IC50 of 27.8 uM, significantly and dose-dependently reduces the protein expression of Skp2 in cancer cells.

T0467 is a small molecule activator of PINK1-Parkin signaling, activates Parkin mitochondrial translocation in dopaminergic neurons and myoblasts (20 uM, 3h), does not induce mitochondrial accumulation of PINK1.

A potent Hsp90 inhibitor with IC50 of 5 nM in cell-free assays.

BX-2819 is a potent, selective Hsp90 inhibitor with KD of 16.4 nM for human Hsp90α, also is a potent B. burgdorferi high-temperature protein G (Bb HtpG) with KD of 12 nM.

DCEM1 is a mitochondrial unfolded protein response (UPRmt) inhibitor, specifically disrupts HSP60-ClpP interaction in PCa cells and in vitro, suppresses prostate cancer growth in vivo.

Foldlin is a small-molecule tool compound that reduces the protein levels of misfolded/aggregated mutant p53, without effect on contact mutants or wild-type p53, Foldlin is small-molecule HSF-1 activator.

HLQ2H (Msi3 inhibitor 2H) is a first-in-class, specific inhibitor of fungal Hsp110 molecular chaperone Msi3, inhibits the holdase activity of Msi3 (IC50=5.02 uM) as well as the growth and viability of C. albicans.

KUNG65 is a potent, selective glucose regulated protein 94 (Grp94) inhibitor with Kd value of 540 nM in fluorescence polarization assays, 73-fold selectivity over Hsp90α.

PLIHZ is a small molecule inhibitor of DNAJA1 derived from the natural compound plumbagin, binds to J domain of DNAJA1 and efficiently reduces the levels of DNAJA1 and several conformational mutp53 with minimal impact on DNA contact mutp53 and wild-type p

PLTFBH is a cell-active small molecule inhibitor of DNAJA1, binds to and reduces protein levels of DNAJA1 and several other HSP40/J-domain proteins (JDPs), specifically reduces conformational mutp53 levels similar to PLIHZ.

SL-145 is a novel C-terminal HSP90 inhibitor, induces apoptosis in TNBC cells via the suppression of oncogenic AKT, MEK/ERK, and JAK2/STAT3 signaling.

SOMCL-16-175 is a non-covalent, allosteric modulator targeting Hsp90α’s middle domain (Hsp90M) with binding Kd of 804 uM, inhibits breast cancer cell growth and proliferation.

STA-1474 is a water soluble prodrug of Ganetespib (STA 9090), which is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).

NW1028 is a small molecule that target the regulatory domain of VCP/p97, inhibits the degradation of a p97-dependent reporter, does not affect the main catalytic domain of p97.

NW1030 is a small molecule that target the regulatory domain of VCP/p97, increases the degradation of a p97-dependent reporter, does not affect the main catalytic domain of p97.

OSSL_325096 is a novel potent small mlolecule p97/VCP inhibitor, suppresses cell proliferation and induces ER stress and apoptotic cell death in MM cell lines (IC50=0.1-0.5 uM).

UPCDC-30766 (UPCDC 30766) is a potent, allosteric inhibitor of AAA+ ATPase p97 (valosin-containing protein, VCP) with biochemical IC50 of 12 nM, EC50 of 226 nM in cellular UbG76V-GFP accumulation assays.

VCP Activator 1 (VA1) is a small molecule allosteric activator of valosin-containing protein (VCP)/p97, dose-dependently stimulates VCP ATPase activity up to 3-fold (EC50= 4 uM).

BT317 is a small molecule dual inhibitor of mitochondrial Lon Peptidase 1 (LonP1) and CT-L proteasome, subsequently induces ROS accumulation and autophagy-dependent cell death in high-grade IDH1 mutated astrocytoma lines.

KDT-11 is a specific, reversible peptidomimetic binder inhibitor of Rpn-13 with binding KD of 3 uM, selectively inhibit proliferation of a broad range of cancer cell lines (NCI60, IC50=5 uM), but not non-malignant cells.

TCL-1 is a non-covalent ligand targeting the Pru domain of Rpn-13, TCL-1 binds to the Pru domain at the Rpn-2 docking site, affects proteasome-mediated proteolysis.

TCL-Ester is the cell-permeable derivative of TCL-1, a non-covalent ligand targeting the Pru domain of Rpn-13.

TXS-8 is a specific, small molecule binder of Rpn-6 with KD of 14 uM, Rpn-6 is a subunit of the 19S regulatory particle (RP) of 26s proteasome.

WZ-1831 is a potent and highly selective inhibitor of human constitutive proteasome chymotryptic activity (β5c) with IC50 of 10 nM, >500-fold selectivity over β5i (IC50=7.1 uM).

ETC-6152 is a potent, specific and covalent E2 ubiquitin ligase UBE2T inhibitor with IC50 of 0.22 uM, targets Cys86 of UBE2T and shows selectivity on UBE2T over UBE2K.

HA-9104 is a specific small molecule inhibitor of E2 conjugating enzyme UBE2F with IC50 of 33.29 uM for inhibition of cullin-5 neddylation, abrogates UBE2F-NEDD8 thioester formation and inhibits cullin-5 neddylation.

UM130646 (UM 130646) is a specific small molecule E2 enzyme UBCH10 inhibitor with IC50 of 20.3 uM in TR-FRET UBCH10 autoubiquitination assays, inhibits UBCH10 E2 activity and antagonizes APC/C-mediated substrate degradation.

YL5084 (YL 5084) is a potent, selective and covalent JNK2/3 inhibitor with IC50 of 70 nM (JNK2), displays selectivity (>30-fold) for JNK2 over JNK1.

BAY-405 is a potent and selective MAP4K1 inhibitor with IC50 of 6 nM. BAY-405 potentiates in vitro and in vivo antitumor T-cell reactivity which overcomes the suppression by TGFβ and PGE2.

F389-0746 is a potent, selective and orally active MAP4K4 inhibitor with IC50 of 120.7 nM.

MMI-0100 is a cell-permeant peptide inhibitor of MAPKAP kinase 2 (MK2), inhibits MK2 and downstream fibrosis and inflammation.

Darizmetinib (HRX-0215, HRX0215) is a potent, selective inhibitor of MKK4 (MAP2K4/SEK1), shows potential for promoting liver regeneration or reducing or preventing hepatocyte death.

DK2403 (DK-2403) is a highly potent, selective and covalent MAP2K7 (MEK7) inhibitor with IC50 of 10 nM, covalently engages the unique Cys218 residue within the active site.

DS03090629 is a potent, selective, ATP-competitive and orally available MEK1/2 inhibitor, shows high affinity for the MEK protein regardless of its phosphorylation status (npMEK (inactive) Kd=0.11 nM, and pMEK (active) Kd=0.15 nM).

HRX-0233 (HRX0233) is a potent, selective MAP2K4 (MKK4) inhibitor, HRX-0233 is synergistic with RAS inhibitors in KRAS-mutant cancers.

KZ-001 is a highly potent and selective MEK 1/2 inhibitor with IC50 values of 7.4/64 nM, respectively, exhibits greater inhibition against BRAF- and KRAS-mutant tumor cells than AZD6244.

NFX-179 (Nedometinib, NFX179) is a potent, specific, topical, metabolically labile MEK1/2 inhibitor with biochemical IC50 of 135 nM (MEK1).

IACS-52825 is a potent, selective dual leucine zipper kinase (DLK, MAP3K12) inhibitor with binding Kd of 1.3 nM, and IC50 of 107 nM in p-c-Jun cell assays.

IKAM-1 (Compound 39-100) is an orally bioavailable, small-molecule IKKβ activation modulator (IKAM) that selectively targets MAP3K1, inhibits TNF-α-induced IKKβ-mediated NF-κB activation in A549 cells with IC50 of 4.7 uM.

KC-130 (KC130, ZAK inhibitor 8) is a potent, selective and covalent leucine-zipper and sterile-α motif kinase (ZAK) inhibitor with IC50 of 11.5 nM.

TC13172 (TC 13172) is a highly potent necroptosis inhibitor targeting the mixed lineage kinase domain-like protein (MLKL), inhibits necroptosis with IC50 of 2 nM in TSZ-induced necroptosis assays in HT-29 cells.

DCZ19931 is a novel multi-targeting kinase inhibitor, exhibits anti-angiogenic effects in vitro and inhibits ocular neovascularization in vivo.

Non-canonical p38α inhibitor NC-37 (NC-p38i NC-37) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM.

Non-canonical p38α inhibitor NC-38 (NC-p38i NC-38) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM.

NuP-3 is a potent, selective MAPK13 and MAPK14 inhibitor with IC50 of 7 and 14 nM, respectively.

VCP979 (VCP-979) is a novel selective small molecule p38 MAPK inhibitor with a significantly greater affinity for the active form of p38 MAPK, has significant anti-fibrotic effects in vitro and in vivo.

IHMT-RAF-128 is a highly potent pan-RAF inhibitor with IC50 of 5.9 and 3.6 nM for BRAF-V600E and CRAF, respectively.

Uplarafenib is a potent, selective small molecule inhibitor of BRAF kinase (IC50=50-100 nM) with antineoplastic activities.

A potent, selective, covalent KRAS G12C inhibitor that selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at sub-micromolar concentrations..

6H05 is a selective, allosteric inhibitor of oncogenic mutant K-Ras(G12C), an intermediate for the synthesis of other oncogenic K-Ras(G12C) inhibitors..

ACA-14 is a small molecule direct inhibitor of KRAS, impedes the interaction of KRAS with its effector Raf and reduces both intrinsic and SOS-mediated nucleotide exchange rates.

ACA22 is a small molecule KRAS inhibitor, inhibits KRAS-mediated signal transduction in cells expressing wild type (WT) and G12D mutant KRAS.

ADT-007 (ADT007) is a potent, specific pan-RAS inhibitor, shows potential to circumvent resistance to mutant-specific KRAS inhibitors and activates antitumor immunity.

ASP6918 (ASP 6918) is a highly potent, covalent KRAS G12C inhibitor with IC50 of 28 nM in cell-free assays, and pERK inhibition IC50 of 3.7 nM in NCI-H1373 cells.

BBO-8956 is a highly potent, covalent inhibitor of GTP-KRAS G12C, BBO-8956 is effective against both GDP and GTP-bound KRAS G12C.

BC-DXI-32982 is a specific small molecule DX2-KRAS inhibitor that specifically binds to the KRAS-binding region of AIMP2-DX2, inhibits interaction between DX2 and KRAS4B with IC50 of 0.18 uM.

CSC01 is a small molecule inhibitor of oncogenic KRAS mutant G13D (KRAS-G13D).

ERAS-5024 (ERAS5024) is a potent and selective KRAS G12D inhibitor with IC50 of 0.86 nM in RAS-RAF binding assays, inhibits ERK1/2 phosphorylation (pERK) formation with IC50 of 2.1 nM in AsPC-1 cell-based assays.

Fulzerasib is a potent selective inhibitor of KRAS gene mutation.

G12Si-5 is a specific small molecule that covalently target K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM.

RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM.

RSC-1255 (KRAS inhibitor 249C, V-ATPase inhibitor) is a Ras-mutant selective cytotoxic agent with nanomolar potency against a spectrum of Ras-mutant cancer cells (A549 (KRASG12S), IC50=73 nM), binds to V-ATPase (Kd=23 nM) and inhibits its activity.

SCH-53239 (SCH53239) is a small molecule inhibitor of Ras nucleotide exchange with IC50 of 0.5 uM, bind competitively with GDP in the nucleotide binding site of the Ras protein.

SIJ1772 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 77 and 96 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively.

SIJ1795 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 82 and 75 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively.

Z640 is a novel non-selective atypical PKC (aPKC) agonist, increases PKCζ and PKCι kinase activity with EC50 of 1.09 and 3.47 µM in vitro kinase activity assays, respectively.

CDD-1115 (CDD1115) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.8 nM and Kiapp of 6.2 nM.

CDD-1281 (CDD1281) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.2 nM and Kiapp value of 8 nM.

CDD-1653 (CDD1653) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 2.8 nM, >360-fold over ALK1, and is inactive versus all other type 1 and type 2 TGFβ family kinases.

Ki26894 (Ki 26894) is a small molecule TGF-beta type I receptor (TbetaR-I) kinase inhibitor, inhibits TGF-β-induced transcriptional activation in MDA-231-D-TβFluc/Rluc cells with IC50 of 0.49 uM.

SRI-31277 is a tripeptide inhibitor of thrombospondin 1 activation of TGF-β, specifically inhibits TGF-β activation mediated through TSP-1 with pIC50 of 8.28 nM.

Ensartinib (X-396) dihydrochloride is a potent, selective and second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with biochemical IC50 of <0.4 nM, inhibits MET with IC50 of 0.74 nM.

Ficonalkib is a potent, selective anaplastic lymphoma kinase (ALK) inhibitor for treating an ALK-mediated disease.

ACP-5862 is a major metabolite of acalabrutinib and potent and selective covalent BTK inhibitor with IC50 of 5 nM.

DZD8586 is an oral, non-covalent, BBB penetrant LYN and BTK dual inhibitor, overcomes resistance mutations to the approved covalent and non-covalent BTK inhibitors.

BLU-808 is a potent and selective wt c-KIT inhibitor, potently inhibits c-KIT–dependent phosphorylation and proliferation with IC50 values in the sub-nanomolar and nanomolar range, respectively.

Dalmelitinib is a potent, selective c-Met tyrosine kinase inhibitor with IC50 of 0.7 nM, inhibits cell growth of gastric cells SNU5 with IC50 of 2.0 nM, binds to the ATP-binding region of c-MET kinase.

Tepotinib (EMD1214063, MSC2156119) is a potent, specific and ATP-competitive inhibitor of MET (HGFR) with IC50 of 23 nM for MET WT autophosphorylation and 2.2-42.6 nM for M1268T, Y1248H, H1112Y, L1213V, H1112L, V1110I, V1206L, and V1238I MET-mutated varia

WM-S1-030 is a highly potent, specific inhibitor of recepteur d'origine nantais (RON kinase, MST1R) with IC50 of 0.39 nM in in vitro enzyme activity.

KI-301690 (KI 301690) is a novel potent, specific DDR1 inhibitor, synergized with gemcitabine to suppress the growth of pancreatic cancer cells.

FC162 is a potent inhibitor of DYRK1A with IC50 of 11, 18, and 68 nM, against DYRK1A, CLK1, and GSK3, respectively.

Leucettinib-21 is a potent, selective DYRKs and CLKs kinases with IC50 of 2.4, 6.7, 12, 33, and 5 nM for DYRK1A, DYRK1B, CLK1, CLK2, and CLK4, respectively.

Y020-3945 is a selective dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor with IC50 of 0.53 uM.

YK-2-69 is a potent, hilghly selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) with IC50 value of 9 nM, shows weak inhibition against DYRK1B (IC50=542 nM) and no activity against DYRK1A/3/4 (IC50>1,000 nM).

An analog of ARRY-380, a potent and selective HER2 inhibitor with IC50 of 8 nM.

A potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.

BI-1622 (BI 1622) is a potent, selective, covalent and orally active HER2 inhibitor with IC50 of 7 nM, potently inhibits HER2 exon 20 mutants while sparing WT EGFR.

BI-4732 is a potent, highly BBB penetrant, fourth-generation EGFR inhibitor against EGFR activating mutations, including C797S.

BI-8128 is a potent, selective, reversible and orally bioavailable fourth generation EGFR inhibitor, potently inhibits oncogenic EGFR variants del19 and L858R as well as the acquired EGFR resistance mutations T790M and C797S.

DSF-102 (DSF102) is a small molecule EGFR inhibitor that interacts with the extracellular domain (ECD) of EGFR, inhibits the interaction with the EGF instead of blocking the intracellular kinase activity, shows inhibition of EGFR dimerization with IC50 of

ER121 (ER-121) is a potent, dual kinase inhibitor targeting both mutant EGFR and activated erbB2 with IC50 of 0.08/0.15 nM (EGFR C797S/EGFR WT, ATP=10 uM).

HCD3514 is a novel potent, selective, fourth-generation EGFR inhibitor targeting C797S triple mutation, strongly inhibits EGFRL858R/T790M/C797S and EGFR19del/T790M/C797S mutations with IC50 of 1.0 and 2.0 nM, respectively.

HNPMI is a small molecule inhibitor of epidermal growth factor receptor (EGFR) with the anticancer potential against various cancers.

HSL119 (HSL 119) is a potent and selective hormonally upregulated neu-associated kinase (HUNK) inhibitor, completely inhibits HUNK kinase activity at 1 uM in biochemical assays.

MTX-241F (MTX241F) is a potent, highly selective and brain-penetrant inhibitor of EGFR, PI3K and DNA-PK with IC50 of 3 nM, 87 nM (PI3Kα) and 5.5 nM, respectively.

OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.

SDT-011 (SDT011) is a small molecule that effectively blocks the binding of anti-EGFR monoclonal antibodies to EGFR, blocks cetuximab-EGFR binding by 62% at 10 uM, binds to EGFR with Kd of 1.7 nM in MST assays.

STX-721 is a potent, selective, next-generation, orally active inhibitor of EGFR exon 20 insertion mutations.

TAS-121 (TAS 121) is an orally available, potent, novel third-generation EGFR-TKI that selectively targets EGFR activating and T790M resistance mutations, sparing wild-type EGFR.

TAS2940 (TAS-2940) is a potent, selective, orally active, irreversible and brain-penetrable pan-ERBB inhibitor.

Targefrin is a potent, selective antagonist targeting ligand binding domain of receptor tyrosine kinase EphA2 (EphA2-LBD), binds to EphA2-LBD with Kd of 21 nM (ITC) and shows IC50 value of 10.8 nM in biochemical assays.

WCDD301 is a high-affinity, orally available agonist of EphA4 receptor.

Irpagratinib (ABSK011) is a potent, selective FGFR4 inhibitor with strong antitumor activity against hepatocellular carcinoma (HCC).

DW14383 is a potent, selective and irreversible inhibitor of FGFR1-4 with IC50 of <0.3 nM, 1.1 nM, <0.3 nM and 0.5 nM for FGFR1/2/3/4 respectively.

Danatinib is a potent and selective FLT3 inhibitor with IC50 of 3 nM, overcomes acquired resistance and shows effective inhibition against FLT3-ITD and/or FLT3-TKD mutations.

MBP-11901 is an orally active, multitarget tyrosine kinase inhibitor targeting FLT3, VEGFR2, PDGFRβ, and c-KIT, shows excellent inhibitory activity against HCC cell growth in vitro (HepG2, IC50=5.16 uM).

PCW-A1001 is a potent, selective inhibitor of FLT-3 (D835Y) mutant with IC50 of 764 nM, weakly inhibits WT FLT-3 with IC50 of 2.54 uM.

TSN084 (TSN 084) is a unique small molecule multi-kinase inhibitor of drug-resistant mutations of c-Met, Trks, and Flt3, also inhibits other oncotargets including Axl, DDRs, and CDK8/19.

YHJ1039 is a broad-spectrum kinase inhibitor, possesses excellent potencies against FLT3 mutants (FLT3 D835Y, IC50=0.41 nM) as well as FAK (IC50=7 nM).

BSJ-04-175 is a potent, selective focal adhesion kinase (FAK, protein tyrosine kinase 2 or PTK2) inhibitor with biochemical IC50 of 22 nM, 30-fold selectivity over PYK2.

BM001 (BM-001) is a small molecular inhibitor of the integral growth hormone/insulin-like growth factor-1 (GH/IGF1) axis, shows potent antiproliferative effect on cancer cells MDA-MM-231 and Colo-205 with IC50 of 20-30 nM.

GTx-134 (GTx 134) is a selective small-molecule inhibitor of IGF-1R and insulin receptor (IR) with biochemical IC50 of 97 nM and 187 nM, respectively.

GNE-4997 is a potent and selective inhibitor of the interleukin-2-inducible T-cell kinase (ITK) with Ki of 0.09 nM.

JTE-051 (JTE051) is a potent, selective inhibitor of interleukin-2-inducible T cell kinase (ITK), suppresses overactive immune response via inhibition of the signal to activate T cells related to immune response.

HSN608 (HSN 608) is a potent inhibitor of RET solvent-front mutants, inhibits RET G810 solvent-front mutants and the V804M gatekeeper mutant with IC50 of <50 nM in cell culture, inhibits ABL1(T315I) with IC50 of 40.7 nM.

The prodrug of TG 100572, a potent, dual receptor tyrosine kinase/Src kinase inhibitor with IC50 of 2-16 nM for VEGFR, FGFR and PDGFR, 0.1-5 nM for Src family.