BI 1342561 is a novel potent and selective SYK inhibitor developed to treat severe asthma.

BI 894416 is a novel potent and selective SYK inhibitor developed to treat severe asthma.

MRL-SYKi is a potent, selective inhibitor of Syk (Spleen tyrosine kinase) with IC50 of <100 nM, also potently inhibits ZAP70 (24 nM in vitro).

MTX-216 (MTX216) is a dual PI3K/EGFR inhibitor that blocks neurofibromin 1 loss of function (NF1LoF) melanoma cell growth in vitro and in vivo, suppresses the activity of SYK kinase with IC50 of 281 nM.

RDN009 (RDN-009) is a potent, selective, and covalent ZAP-70 kinase inhibitor with IC50 of 55 nM.

RDN2150 is a potent, selective and covalent ZAP-70 inhibitor with IC50 of 14.6 nM, shows no significant activity against Syk, covalently binds to the C346 residue of ZAP-70.

Adrixetinib is a small molecule inhibitor of Axl/Mer RTK.

ER851 (ER-851) is a potent and highly selective AXL inhibitor.

INCB081776 is a potent and selective dual inhibitor of AXL and MERTK with IC50 of 16 and 14 nM respectively, 30-fold selectivity over TYRO3.

R992 (MERTK inhibitor) is a novel potent, selective and orally bioavailable inhibitor of Mer tyrosine kinase (MerTK) with IC50 of 18 nM in ADP-Glo assays.

UNC2025 is a potent, orally bioavailable Mer/FLT3 dual inhibitor with IC50 of 0.74/0.8 nM, 700-fold less active against Met compared to Mer.

Anizatrectinib is a potent and orally active inhibitor of TrkA kinase with potential for inflammatory disease such as prostatitis.

Emzeltrectinib is a potent, selective neurotrophic factor tyrosine kinase receptor TrkB inhibitor, shows potential for treatment of Trk kinase-mediated tumor.

PTX-BD10-2 (BD10-2) is a selective, brain-penetrant small molecule TrkB/C receptor partial agonist, shows survival-promoting activity.

COB223 is a chemical inhibitor of angiogenesis and tumorigenesis, targets the VEGF signaling pathway upstream of Ras, inhibits endothelial cell migration with IC50 of 5 uM.

NRP1-4 (Neuropilin 1-4) is a highly potent, specific small molecule inhibitor of VEGF-A binding to neuropilin 1 (NRP1) with IC50 of 0.598 nM, reduces calcium and sodium currents through binding to NRP1 and inhibits the effects of VEGF-A.

NRPa-308 is a neuropilin-1 (NRP-1) antagonist, inhibits the VEGF-A165/NRP-1 binding with IC50 of 42 uM, exerts in vitro anti-angiogenic activity.

SYHA1813 is a potent dual inhibitor of CSF1R and VEGFR with IC50 of 19.3, 2.8, 0.3, and 4.3 nM for CSF1R, VEGFR1, 2, and 3, respectively.

CW85319 is a small-molecule compound that enhances Axin2's interaction with GSK3β, shows a high-affinity binding with Axin2 with Kd of 5.8 uM.

iCRT-3 is a selective, cell-permeable β-catenin responsive transcription (CRT) inhibitor with IC50 of 8.2 nM.

IMU1003 (IMU-1003) is a small molecule inhibitor of Wnt/β-catenin signaling, decreases β-catenin levels and inhibits target gene expression that promotes cancer cell proliferation.

AB668 is a selective, bivalent Casein Kinase 2 (CK2) inhibitor targeting the ATP site and the αD pocket, AB668 inhibits the CK2 holoenzyme with Ki value of 41 nM (IC50=65 nM).

CKR-49-17 is a potent, allosteric small molecule activator of CK1γ2 with Kd value of 180 nM in MST assays.

FL-1607 is a novel Fam20C inhibitor with potent anti-proliferative effects on TNBC cells, induces apoptosis and inhibits migration in MDA-MB-468 cells.

SGC-CK2-1 analog 2h is potent, selective and in vivo active inhibitor of casein kinase 2α (CSNK2A, CK2α) with pIC50 of 7.5 and 7.7 against CSNK2A1 and CSNK2A2, respectively.

SR-4133 (SR4133) is a potent and highly selective CK1ε isoform inhibitor with IC50 of 58 nM, no significant acitivity agianst CK1δ (IC50>10,000 nM).

BMD4702 is a small molecule Dishevelled (Dvl) PDZ domain with binding Kd of 186 nM.

BMD4722 is a highly potent, small-molecule inhibitor of Dvl-CXXC5 interaction with IC50 of 2.59 uM, directly binds to the Dvl PDZ domain (Kd=22.3 uM).

NPL-4011 is a specific small molecule inhibitor of PDZ domain of human Dvl1 (Dvl1-PDZ) with KD vaule of 34.5 uM in NMR titration experiments.

MDB5 is a potent hedgehog (Hh) signaling pathway inhibitor, exhibits stronger inhibition of the Hh pathway and anticancer effect in vitro and vivo than GDC-0449.

Picoberin is a highly potent (low picomolar) inhibitor of purmorphamine- and Sonic Hedgehog (Shh)-induced osteogenesis with IC50 of 3 pM, acts as an AhR agonist and induces the expression of AhR target genes, thereby suppressing osteoblast differentiation

aNDR1 (NDR1 agonist) is a specific small-molecule agonist of Nuclear Dbf2-related kinase 1 (NDR1, STK38), specifically inhibits CRPC cells and promotes kinase activity of NDR1.

TRULI is a small molecule Yap signaling activator, acts as an ATP-competitive inhibitor of Lats kinases in vitro (Lats1 kinase, IC50=0.2 nM, 10 uM ATP), prevents Yap phosphorylation in the cell-based assays with EC50 of 510 nM.

UNC-BE4-017 is a selective STK3 small-molecule inhibitor, also potently inhibits JAK1, JAK2, and JAK3, but not other kinases in a panel of 48 kinases.

UNC-SOB-5-16 is a potent, selective STK3 small-molecule inhibitor with IC50 of 22 nM, also inhibits LRRK2.

AG-1031 (AG1031) is a specific small molecule inhibitor of the double-stranded DNA binding activity of positive coactivator 4 (PC4) with IC50 of 2.5 uM, more effectively than its single-stranded DNA binding activity (IC50=15 uM).

Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC).

MRT-92 is a potent selective Smoothened (Smo) receptor antagonist (Kd=0.3 nM), inhibits rodent cerebellar granule cell proliferation induced by Hh pathway activation with IC50 of 0.4 nM.

INS018_055 (INS018-055) a selective small-molecule TRAF2- and NCK-interacting kinase (TNIK) inhibitor with Kd value of 4.32 nM and IC50 of 31 nM, inhibits TGF-β-induced α-SMA protein expression in MRC-5 cells with IC50 of 27.14 nM.

C644-0303 is a novel Wnt/β-catenin signaling inhibitor (IC50=4.2 uM) with antitumor efficacy, inhibits both constitutive and ligand activated Wnt signals and its downstream gene expression.

ISQ-1 is a potent in vitro inhibitor of several cancer cell lines (LS174T cell proliferation, IC50=100 nM), inhibits Wnt signaling and also activates adenosine monophosphate kinase (AMPK).

LPD-01 is a small molecule inhibitor of the Wnt/β-catenin signaling pathway, directly binds to importin7, inhibits the transactivation of target genes of the Wnt/β-catenin signaling pathway.

WNTinib is a multi-kinase inhibitor with specificity against β-catenin (CTNNB1) mutant hepatocellular carcinoma, harnesses the KIT/MAPK/EZH2 pathway, shows durable and selective transcriptional repression of mutant β-catenin/Wnt targets through nuclear tr

A potent, selective γ-secretase inhibitor that significantly reduces the right ventricular systolic pressure and right heart hypertrophy in hypoxia/SU5416 (SUHx) rats..

RXC004 (RXC-004) is a potent, selective Porcupine (PRCN) inhibitor, inhibits functional Wnt production from mouse L-Wnt3a cells with IC50 of 64 pM in luciferase reporters assays.

WHN-88 is a potent, selective Porcupine (PORCN) inhibitor, inhibits Wnt/β-catenin signaling with IC50 of ST-Luc of 0.02 uM.

ZD06519 is a novel camptothecin payload for antibody drug conjugates (ADCs) with highp ayload potency (~1 nM).

A drug-linker conjugate for antibody-drug conjugate by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide SuO-Val-Cit-PAB..

EN106 derivative 1 is a EN106 derivative used for PROTAC design, EN106 is a covalent ligand and recruiter for FEM1B E3 ligase for targeted protein degradation.

EN106 derivative 2 is a EN106 derivative used for PROTAC design, EN106 is a covalent ligand and recruiter for FEM1B E3 ligase for targeted protein degradation.

Thalidomide-O-PEG4-Acid is a chemical linker for PROTAC design.

(R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM.

ARD-1676 (ARD1676) is a highly potent and orally efficacious PROTAC degrader of the androgen receptor (AR) with DC50 values of 0.1 and 1.1 nM in AR+ VCaP and LNCaP cell lines, respectively.

BI 1810284 (ACBI2, BI 01810284) is a potent, selective and orally bioavailable VHL-recruiting PROTAC degrader of SMARCA2 (DC50=1 nM in RKO cells), 30-fold selectivity over SMARCA4.

BJG-05-039 is a PAK1-selective degrader consisting of NVS-PAK1-1 conjugated to lenalidomide, a recruiter of the E3 ubiquitin ligase substrate adaptor Cereblon.

BSJ-04-146 is a potent, selective FAK PROTAC (IC50=26 nM), induces potent and durable FAK degradation in pancreatic and breast cancer cell lines at 10 nM.

BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78.

BTX-6654 is a potent, selective SOS1 cereblon-based bifunctional PROTAC degrader, reduces downstream signaling markers, pERK and pS6, and displayed antiproliferative activity in cells harboring various KRAS mutations.

BWA-522 is a potent, orally bioavailable PROTAC degrader of the androgen receptor N-terminal domain (AR-NTD), induces AR-FL or AR-V7 protein degradationwith DC50 of 0.73 μM (AR-FL) and 0.67 μM (AR-V7) in VCaP cells.

CC-3240 is a molecular glue degrader of CaMKK2 based on CC-8977 with bingding IC50 of 9 nM and DC50 of 100 nM (THP1 cells, Dmax=92%).

Chk1 PROTAC-2 is a potent Chk1 degrader with DC50 of 1.33 µM in A375 cells.

CRBN(BRAF)-24 is a potent small molecule degrader against oncogenic BRAF V600E protein, potently degrades BRAFV600E in a ubiquitin–proteasome system (UPS)-dependent manner and inhibits the proliferation of BRAFV600E-driven cancer cells.

CRBN(FLT3)-8 a highly potent FLT3 degrader by introducing gilteritinib into targeted protein degradation technology, potently degrades FLT3-ITD via UPS and inhibits the proliferation of FLT3-ITD mutant AML cells more effectively than gilteritinib.

DAS-5-oCRBN is a potent and selective PROTAC for c-Src kinase with DC50 value of 3 nM, without effect on Bcr-Abl.

DAS-CHO-5-oCRBN is a potent and selective PROTAC for c-Src kinase with DC50 value of 62 nM in CAL148 cells.

DB0614 is a CRBN-based PROTAC, induces the degradation of NEK9, FAK, CDK4, CDK6, and WEE1 in cells.

DBt-10 is a potent BTK-specific DCAF1 PROTAC with TR-FRET IC50 of 136 nM, potently degrades BTK with DC50 of 137 nM in TMD8 BTK-GFP/mCherry cell-based assays.

dEALK1 is a small-molecule degrader of EML4-ALK fusion proteins with binding constant (Kd) value of 44 nM for kinase domain of recombinant ALK, overcomes resistance to ALK inhibitor ceritinib.

DeFer-2 is an oleic acid (OA)-based ferritin-targeting PROTAC binding Kd of 17.1 uM, degrades ferritin and rapidly elevates the free iron content, induces pyroptosis.

Degradomer D-1 is a selective proteasomal degrader of IRAK3 with Kd of 100 nM, DC50 of 94 nM, displays no binding affinity against IRAK4 (Ki >10 uM).

DU-14 is a highly potent and selective small molecule degrader for both PTP1B and TC-PTP with DC50 values of 4.3 and 4.8 nM, respectively, in HEK293 cells after 16 hours treatment.

GNE-0011 is a monovalent, JQ1-based BRD4 degrader that is not linked to an E3 ligase binder, triggers proteasomal and ubiquitin-dependent selective degradation of BRD4 over BRD2 and BRD3.

HDAC3 PROTAC P7 is a potent and selective HDAC3-directed PROTAC with IC50 of 40 nM (HDAC3 deacetylase activity), effectively induces HDAC3 degradation with DC50 of 0.6 nM in THP-1 cells (Emax=90%).

HJM-561 is a potent, selective and orally bioavailable EGFR PROTAC degrader, selectively degrades the EGFR C797S-containing triple mutants Del19/T790M/C797S and L858R/T790M/C797S with DC50 values of 9.2 nM and 5.8 nM, respectively.

HPP-9 is a potent BET bromodomain degrader that acts through a PROTAC mechanism, HPP-9 is a long-acting Hedgehog pathway inhibitor.

INY-06-061 is a potent and selective heterobifunctional degrader of ERK5 with binding Kd of 12 nM and DC50 of 21 nM in MOLT4 cells (5h treatment).

JCS-1 is a RG3039-based degarder (PROTAC) of the RNA decapping scavenger protein DcpS exhibiting effective degradation of DcpS at nanomolar concentrations, non-covalently binds DcpS and recruits the E3 ligase VHL, induces potent, rapid, and sustained DcpS

JET-209 (JET209) is a potent, selective PROTAC degrader of CBP/p300 based on GNE-207 with DC50 of 0.05 nM for CBP and 0.2 nM for p300, Dmax >95% for both proteins in the RS4;11 leukemia cell line.

JH-XII-03-02 is a highly potent, selective PROTAC degrader of LRRK2 with IC50 of 1 nM against both wt LRRK2 and LRRK2 G2019S.

JWZ-1-80 is a potent and selective PROTAC degrader of PI5P4Kγ with Kd of 510 nM, 1 uM induces 75% reduction of PI5P4Kγ in Molt4 cells.

KH-103 is a highly potent, catalytically-driven glucocorticoid receptor (GR) PTORAC degrader, demonstrate excellent performance in passively preventing ligand-induced gene expression activation in the absence of partial agonistic transcriptional triggerin

KYH1872 is a PROTAC that induces protein degradation via the KLHDC2 E3 ubiquitin ligase, KYH1872 is consisted of a C-terminal fragment of the SelK protein and promiscuous kinase inhibitor YHJ1039 via PGE linker.

LL-K8-22 is a potent, selective dual degrader of of CDK8 and cyclin C (MDA-MB-468 cell DC50, 2.52 and 2.64 uM), significantly degrades CDK8 without reducing CDK19 and does not degrade other cyclin proteins.

MS132 is a highly potent and selective VHL-recruiting WDR5 PROTAC degrader with DC50 of 92 nM in MIA PaCa-2 cells.

MS147 (MS 147) is the first degrader of PRC1 core components, BMI1 and RING1B, comprises an EED small-molecule binder (EED226, Cat. PC-42321) linked to a ligand of the E3 ligase von Hippel-Lindau (VHL), degrades BMI1/RING1B in an EED-, VHL-, ubiquitinatio

MS3227 is a proteolysis-targeting chimera (PROTAC) that targets MDM2 by recruiting the E3 ligase VHL, resulting in proteasome-dependent degradation of MDM2.

MTX-23 is a proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) splice variant-7 (AR-V7) and AR-full length (AR-FL) with DC50 of 0.37 and 2 uM, respectively.

PIK5-12d is a highly potent, selective, first-in-class PIKfyve PROTAC degrader, potently degrades PIKfyve protein with DC50 value of 1.48 nM and Dmax value of 97.7% in prostate cancer VCaP cells.

PROTAC dCE-1 is a potent, selective CBP/EP300 degrader targeting the histone acetyltransferase (HAT) domain, with DC50 value of 1.3 μM in LP1 cells.

PTD10 is a highly potent BTK PROTAC degrader with DC50 of 0.5 nM in TMD8 cells, inhibits cell growth and induces apoptosis more potently than parent molecule GDC-0853.

QA-68-ZU81 (QA-68) is a EA-89-based BRD9 degrader that incorporates the EA-89 warhead into a cereblon (CRBN)-targeting proteolysis-targeting chimera (PROTAC).

SelDeg51 (Selective Degrader of FKBP51) is a potent, selective FKBP51 PROTAC with Kd of 18 nM, Emax=90%.

TD-802 is potent, cereblon-mediated androgen receptor PROTAC degrader, effectively inducs AR protein degradation with DC50 of 12.5 nM and Emax 93% in LNCaP prostate cancer cells.

TMX-2172 is a potent, selective CDK2 and CDK5 dual PROTAC degrader with IC50 of 6.5 nM and 6.8 nM for CDK2/cyclin A and CDK5/p25, respectively.

TMX-4153 (TMX4153) is a bivalent PIP4K2C degrader (MOLT4 cells, DC50=24 nM, Dmax=921% at 1 uM) based on TMX-4084, rapidly and selectively degrades endogenous PIP4K2C.

U7D-1 is a selective USP7-degrading Proteolysis Targeting Chimera (PROTAC). U7D-1 showed selective and effective USP7 degradation, and maintained potent cell growth inhibition in p53 mutant cancer cells.

UBX-382 (UBX382) is a potent and orally available proteolysis-targeting chimera (PROTAC) that induces potent BTK degradation in DLBCL cell line with DC50 of 4.5 nM.

UNC7700 (UNC-7700) is a potent EED-targeted PRC2 degrader, contains a unique cis-cyclobutane linker and potently degrades all PRC2 components EED (DC50=111 nM; Dmax=84%), EZH2WT/EZH2Y641N (DC50=275 nM; Dmax=86%) and SUZ12 (Dmax=44%) in DLBCL cells.

WD6305 is a potent and selective proteolysis-targeting chimera (PROTAC) degrader of METTL3-METTL14 complex with DC50 of 140 nM (METTL3), Dmax of 91.9% in Mono-Mac-6 AML cell line.

MS40 is a cereblon (CRBN)-based proteolysis targeting chimera (PROTAC) degrader of the onco-target WD repeat domain 5 (WDR5) [1]. WDR5 is an integral component of the MLL/KMT2A lysine methyltransferase protein complex. The WDR5-binding component of MS40 is the selective inhibitor OICR-9429, and the CRBN-targeting moiety is the immunomodulatory drug pomalidomide. MS40 promotes degradation of WDR5 and the pomalidomide transcription factor neo-substrates IKZF1 and IKZF3.

XY-07-35 is a potent, selective HDAC6 proteolysis targeting chimera (PROTAC) degrader with IC50 of 48.5 nM.

YX968 is a potent, selecive HDAC3/8 dual PROTAC degrader with DC50 of 1.7 and 6.1 nM in degrading HDAC3 and HDAC8 respectively (MDA-MD-231 cell, 8 h).

ZZ151 (ZZ-151) is a highly potent and selective SOS1 degrader PROTAC with DC50 of 15.7 nM (Dmax=100%).

AdipoAI is a novel small molecule APN receptor (AdipoR, adiponectin receptor) agonist.

ALY688 (ADP 355) is an adiponectin mimetic adiponectin receptor (AdipoR) agonist, inhibits the growth of AdipoR1/AdipoR2-positive cancer cell lines (MCF-7 cell, 0.1-10 uM).

K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals.

Wyeth-1 (hAMCase inhibitor 1) is a potent, selective inhibitor of human acidic mammalian chitinase (hAMCase) with IC50 of 210 nM, 20-fold selectivity over hCHIT1.

DL5050 (DL 5050) is a potent selective agonist of human constitutive androstane receptor (CAR) with EC50 of 0.37 uM in cell-based luciferase reporter assays (Emax=3.8).

DL7076 (CN06) is a small molecule dual activator of the constitutive androstane receptor (CAR, NR1I3) and nuclear factor erythroid 2-related factor 2 (Nrf2) with EC50 of 8.85 and 0.72 uM, respectively.

BVT173187 is a potent, selective, non-peptide inhibitor of formyl peptide receptor 1 (FPR1), inhibits fMLF and WKYMVM induced oxidase activity.

ICT12035 (AZ2158) is a potent, selective formylpeptide receptor-1 (FPR1) antagonist with IC50 of 30 nM in calcium mobilisation assays (100 nM fMLF).

MD102 is a potent transglutaminase 2 (TGase 2; TG2) inhibitor with IC50 of 0.35 uM, shows p53 stabilization effect and anticancer activity at RCC cell lines.

ZED1227 is a potent, selective, covalent, and orally active transglutaminase 2 (TGase 2, TG2) inhibitor with IC50 of 45 nM.

LJ4827 (LJ-4827) is a potent, specific inhibitor of HASPIN, a mitotic kinase for Histone H3, with Ki value of 0.46 nM, enzyme IC50 of 0.155 nM in HASPIN kinase assay performed with Histone H3 peptide.

AG-120-X is a first-in-class small molecule inhibitor of ICOS/ICOSL interaction with IC50 of 4.68 uM in TR-FRET assay, dose-dependently blocks ICOS/ICOSL interaction in cellular assay based on co-culturing Jurkat T cells expressing ICOS and CHO-K1 cells e

C-5401331 is a small molecule T-cell immunoglobulin and mucin domain-containing protein 3 (Tim-3) inhibitor, suppresses acute myeloid leukemia (AML) cell proliferation.

L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth.

MTX-3937 is a small-molecule Siglec-9 inhibitor with binding KD of 3.15 uM in BLI assay, inhibits phosphorylation of Siglec-9 and downstream SHP1 and SHP2.

ARUK3001185 is a potent, selective, brain-penetrant inhibitor of Wnt-deactivating enzyme Notum carboxylesterase activity with IC50 of 6.7 nM in OPTS biochemical assay.

LP-914822 (LP914822) is a potent, selective and orally-active NOTUM with IC50 of 2 nM for human, mouse and rat Notum.

LP-935001 (LP935001) is a potent, selective and orally-active NOTUM with enzyme IC50 of 0.4 nM for both of human and mouse Notum.

AS-48 is a specific, small-molecule measles virus (MeV) entry inhibitor with IC50 of 0.6 uM agianst MV-KS.

MBZM-N-IBT is a small molecule inhibitor of Chikungunya virus (CHIKV), inhibits CHIKV infection in vitro in RAW 264.7 cells with IC50 of 22.34 uM, targets CHIKV nsP2 protease activity.

SBI-0090799 (SBI 0090799) is a selective and potent inhibitor of Zika virus (ZIKV) replication, inhibits replication of multiple ZIKV strains and in different cell systems.

UMM-766 is an orally available nucleoside analog with potent, broad-spectrum antiviral activity against multiple members of orthopoxviruses (EC50<1 uM against VACV).

USC-373 is a phosphonate prodrug of HPMPC (cidofovir) with activity against VZV and other DNA viruses.

EOS789 is a potent, pan-phosphate transporter inhibitor, inhibits phosphate uptake in a noncompetitive manner for human NaPi-IIb, PiT-1, and PiT-2 with IC50 of 6.8, 1.5 and 1.7 uM, respectively.

EOS789 tosylate is a potent, pan-phosphate transporter (NaPi-2b, PiT-1, PiT-2) inhibitor, inhibits phosphate uptake in a noncompetitive manner for human NaPi-IIb, PiT-1, and PiT-2 with IC50 of 6.8, 1.5 and 1.7 uM, respectively.

LY3358966 is a potent, selective inhibitor of the intestinal sodium-dependent phosphate cotransporter NPT2b (NaPi-2b, SLC34A2), inhibits phosphate uptake in human NPT2b expressed in CHO cells with IC50 of 32.4 nM.

TY-2136 is a next generation ROS1/TRK/ALK inhibitor with IC50 of 1.6 nM and 460.1 nM for ROS1 G2032R and TRKA G595R, respectively, inhibits ROS1/TRK/ALK mutations and overcomes drug resistance due to acquired solvent-front mutations.

1D-142 is a novel small molecule RHO family of GTPase RAC1 inhibitor, inhibits Rac1-GEF interaction and reduces Rac1-mediated TNFα-induced NF-κB nuclear translocation during cell proliferation and migration.

CS7171 is an effective, blood-brain barrier (BBB) permeable small molecule inhibitor of hippocampal Rac1 activity, rescues learning deficits in APP/PS1 mice.

GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.

JKF-034 is an effective,blood-brain barrier (BBB) permeable small molecule inhibitor of hippocampal Rac1 activity, rescues learning deficits in APP/PS1 mice.

PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.

BAY 2686013 is a selective, allosteric antagonist of human pituitary adenylate cyclase activating polypeptide receptor (hPAC1-R) with IC50 of 0.92 and 0.4 uM in cAMP HTRF and Ca2+ release assays, respectively.

PA-915 (PA915) is a small-molecule, non-peptide antagonist of the PACAP type I (PAC1) receptor, inhibits PACAP (1 nM)-induced phosphorylation of CREB in PAC1/CHO cells with IC50 of <10 pM.

Ro 25-1553 is a potent, selective VIPR2 agonist and a cyclic peptide analog of vasoactive intestinal peptide (VIP), displaces the radioligand 125I-VIP from rat forebrain membranes with IC50 of 4.98 nM.

AF-2112 is a small molecule inhibitor of TEAD, reduces the expression of CTGF, Cyr61, Axl and NF2, inhibits migration of human MDA-MB-231 breast cancer cells.

LM98 (TEAD inhibitor LM98) is a flufenamic acid analogue, shows strong affinity to TEAD, inhibits its autopalmitoylation and reduces the YAP-TEAD transcriptional activity.

mCMY020 is a potent, specific and covalent inhibitor of TEAD transcriptional activity with IC50 of 91.9-468.6 nM for TEAD1-4.

MYF-03-69 is a selective, covalent, irreversible TEAD inhibitor, binds with TEAD palmitate pocket, disrupts YAP-TEAD association, suppresses TEAD transcriptional activity (IC50=45 nM) and inhibits cell growth of defective Hippo signaling.

NSC682769 is a specific YAP-TEAD signaling inhibitor, blocks the association of the YAP and TEAD interaction interface, directly binds to YAP with Kd of 738 nM.

PDHPS1 is an endogenous stable peptide which is derived from the C-terminal (2090-2110) of NUMA1, inhibits the proliferation of ovarian cancer cells in vitro, regulates ovarian cancer development through targeting YAP1 signaling, binds to and interacts wi

SWTX-143 is a potent, irreversible and covalent YAP/TAZ-TEAD inhibitor with IC50 of 12 nM in luciferase reporter assays, binds to the palmitoylation pocket of all four TEAD isoforms, inhibits Hippo pathway-mutant cancer cells.

TAT-PDHPS1 is an endogenous stable peptide that inhibits the proliferation of ovarian cancer cells in vitro, regulates ovarian cancer development through targeting YAP1 signaling, binds to and interacts with protein phosphatase 2 phosphatase activator (PT

TEAD activator Q2 (Quinolinol Q2) is a small molecule activator of TEAD with EC50 of 2.6 uM in TEAD dual-luciferase reporter (DLR) assays, inhibits TEAD-palmitate interaction with IC50 of 1.7 uM.

TED-642 (TED642) is a potent, covalent, pan-TEAD-YAP1 antagonist, inhibits TEAD1/2/4 binding to YAP with IC50 of 0.9-1.2 uM.

VT-107, as an analogous to VT104, is an orally active and potent pan-TEAD auto-palmitoylation inhibitor. VT-107 can be used for the research of cancer.

EIDD-1931 (Beta-d-N4-hydroxycytidine, β-d-N4-hydroxycytidine, NHC) is an active metabolite of EIDD-2801 with broad-spectrum antiviral inhibitor of SARS-CoV-2.

Thioparib is a next-generation potent, orally bioavailable pan-PARP inhibitor with IC50 of 0.13/0.006 nM (PARP1/2), overcomes multiple PARPi resistance both in vitro and in vivo.

Zenuzolac (GLS1027, VGX-1027) is a small molecule immunosuppressant and an orally available isoxazole compound, inhibits toll-like receptor 4 (TLR4) activity, has shown promise for the treatment of several neuroinflammatory disorders.

VPC-80051 (VPC80051) is the first small molecule inhibitor of hnRNP A1 splicing activity, targets RNA-binding domain (RBD) of hnRNP A1.

PF-719 (PF719) is a potent, selective Pyk2 inhibitor with IC50 of 17 nM, displays 25-fold selectvity over FAK (IC50=469 nM).

DEG-77 is a cereblon-dependent degrader of IKZF2 and casein kinase 1α (CK1α). It blocks cell growth and delays leukemia progression in murine and human acute myeloid leukemia (AML) mouse models.

T1-44 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It exhibits anti-tumor activity in pancreatic cancers.

LY3537982 (KRAS G12C inhibitor 19) is a highly selective and potent inhibitor of the  KRAS-G12C protein. LY3537982 selectively inhibits the growth of KRAS G12C mutant cells H23 G12C, H358 G12C, and H2122 G12C with IC50s of 1.04 nM, 1.16 nM, and 11.38 nM, respectively.

MSU-42011 is an orally active agonist of retinoid X receptor (RXR). MSU-42011 inhibits the expression of iNOS and p-ERK protein. It exhibits immunomodulatory and antitumor activity. MSU-42011 can be used for cancer research.

Fluorofurimazine is a novel furimazine analogue, with increased aqueous solubility enabling higher signal emission than furimazine for bioluminescence imaging. Fluorofurimazine enables higher substrate loading and improved optical imaging sensitivity in in-vivo.

L-Cysteine hydrochloride hydrate is an essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione, and taurine. L-Cysteine hydrochloride hydrate suppresses ghrelin and reduces appetite in rodents and humans.

L-Cystine dihydrochloride is used as a cell culture media component for the commercial biomanufacture of therapeutic recombinant proteins and monoclonal antibodies and as a sulfur-containing precursor of glutathione (GSH) synthesis. L-Cystine dihydrochloride homeostasis is also important for GSH functions.

NADP sodium salt, a nicotinamide adenine dinucleotide, is a coenzyme that plays a vital role in various metabolic reactions within living cells. NADP sodium salt is a key cofactor for electron transfer in the metabolism, being alternately oxidized (NADP+) and reduced (NADPH).

Sodium alginate is a sodium salt of alginic acid, can be extracted and purified from the cell walls brown seaweed Laminaria japonica. It has chelating activity and can be used to adsorb heavy metal ions, also has mucosal-protective and hemostatic effects and used in food additives and pharmaceuticals.

Sodium Montmorillonite is a layered clay mineral (2:1 phyllosilicate) that belongs to a class of the smectite group. It can be used for preparation of new drug delivery systems, especially for slow release of protonable drugs due to its high degree of surface area and high capacity for cation exchange.

ALKBH5 inhibitor (Cpd 20m) is a potent and selective inhibitor of RNA m6A demethylase AlkB homolog 5 ALKBH5 with IC50 of 21 nM.

ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP). It exhibits an EC50 of 1.37 μM for α-casein hydrolysis by HsClpP. ZK53 treatment allosterically activates HsClpP to uncontrollably degrade the essential mitochondrial proteins and is inactive toward bacterial ClpP proteins.

LY2880070 is an orally active inhibitor of CHK1. LY2880070 can be used as an anticancer agent and shows promise in preclinical models of pancreatic ductal adenocarcinoma (PDAC) when used in combination with DNA-damaging agents.

N6F11 is a ferroptosis inducer, and can trigger the degradation of glutathione peroxidase 4 (GPX4) specifically in cancer cells. N6F11 can be used for ferroptosis study.

Pyrimidine is an endogenous metabolite. It is used to study the photoinduced ion chemistry of the halogenated pyrimidines, a class of prototype radiosensitizing molecules, and is also used to assess pyrimidine/purine asymmetry quantitatively.

XST-14 is a potent, competitive, and highly selective inhibitor of ULK1 and exhibits an IC50 of 26.6 nM in an in vitro ULK1 kinase activity assay, respectively. XST-14 reduces the phosphorylation of the ULK1 downstream substrate and induces autophagy inhibition. It exhibits antitumor effects.

FL118(10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin analog, is a potent and orally active inhibitor of Survivin. FL118 also selectively and independently inhibits three additional cancer-associated survival genes Mcl-1, XIAP, and cIAP2 in a p53 status-independent manner. FL118 displays potent antitumor activity and can be used in cancer research.

p-Toluic acid (4-Methylbenzoic acid) is a methylbenzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc. It also exhibits hepatotoxicological potential in humanised-liver mice.

Protokylol hydrochloride(Caytine hydrochloride, JB-251 hydrochloride) is a salt form of protokylol and is an agonist of β-adrenergic receptor. Protokylol hydrochloride is also used as a bronchodilator.

Coenzyme Q1 (CoQ1) is localized to the hydrophobic domain of the phospholipid bilayer of mitochondria, plasma lipoproteins, and other biological membranes. CoQ1 reduction has a strong rotenone-insensitive component and can be used to measure the mitochondrial respiratory chain complex 1 activity.

Thiorphan (DL-3-Mercapto-2-benzylpropanoylglycine) is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM. It is also a potent inhibitor of enkephalinase, with antinociceptive activity.

ACT001(DMAMCL, dimethylaminomicheliolide) is a PAI-1 inhibitor and exerts antitumor effects on neuroblastoma (NB) both in vitro and in vivo. It also exerts synergistic effects in combination with cisplatin through the inhibition of the PAI-1/PI3K/AKT pathway.

EGTA tetrasodium(Ethylene glycol-bis(β-aminoethyl ether)-N,N,N',N'-tetraacetic acid tetrasodium salt) is a calcium chelator, used for the determination of calcium in the presence of magnesium. EGTA tetrasodium significantly inhibits the substrate adherence capacity of inflammatory macrophages.

Deutenzalutamide (HC-1119, MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. It can be used in a treatment of advanced prostate cancer.

Zilurgisertib fumarate(INCB-000928 fumarate, NBU-928 fumarate) is a selective ALK 2 inhibitor.It is under development for the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.

3,3-Dimethyl-1-butanol (Neohexanol) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-dimethyl-1-butanol negatively inhibits the signalling pathways of p65 NF-κB and  TGF-β1/Smad3. 3,3-dimethyl-1-butanol has potential applications in cardiovascular disease (CVD).

Fasoracetam (NS 105) is a metabotropic glutamate receptor activator with a potential to treat vascular dementia.

Ethotoin (Peganone) is a hydantoin derivative and an orally active anticonvulsant agent. It also exerts an antiepileptic effect and can be used in epilepsy research.

Lotiglipron (PF-07081532) is an orally active GLP-1R agonist. It reduces glucose and body weight, and has the potential to be used in Type 2 diabetes mellitus (T2DM) research.

Solutol HS-15(Polyethylene glycol 12-hydroxystearate) is a Macrogol 15 hydroxy stearate, which improves permeability by disrupting the membrane structure/fluidity change.

Potassium clavulanate cellulose (Potassium clavulanate:cellulose (1:1)) is a mixture of potassium clavulanate and cellulose, is a bacterial β-lactamase inhibitor. Potassium clavulanate with the combination of amoxicillin can be used for the research of different infections caused by bacteria, such as sinusitis, pneumonia, ear infections, bronchitis, urinary tract infections, and infections of the skin.

2,4-Thiazolidinedione (Thiazolidinedione), an insulin sensitizer, is a specific agonist of peroxisome proliferator-activated receptor (PPAR)γ. Thiazolidinedione treatment corrects impaired muscle insulin action in vivo.

Biotin-(L-Thyroxine) is the biotinylated L-Thyroxine. L-Thyroxine is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from Biotin-(L-Thyroxine) (T4).

EDI048 (compound 1.16) is an orally active Cryptosporidium PI4K inhibitor for the research of cryptosporidiosis.

Enavermotide (UCP2) is an immunological agent for active immunization (antineoplastic).

Sucantomotide is an immunological agent for active immunization (antineoplastic).

Zelenectide (BCY8116) is a Bicycle peptide targeting to Nectin-4, which is a cell adhesion molecule. Zelenectide serves as a Bicycle tumor-targeted immune cell agonist.

9-Deazaguanine is a nucleoside analog with potent inhibitory activity against purine nucleoside phosphorylase (PNP).

XY-52 (Compound 32) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 5.68 μM in AlphaLISA assay, and 4.59 μM in HEK-Blue assay. XY-52 increases proinflammatory T-cell proliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model.

Civorebrutinib (WS-413) is a Bruton's tyrosine kinase inhibitor with antineoplastic effect.

Tegomil fumarate is an immunomodulator.

Ucasareotide dasaroxetan (SarTATE) is diagnostic agent with antineoplastic effect.

BC-05 is an orally active and potent inhibitor of CD13 and proteasome. BC-05 has an IC50 value of 0.13 μM for human CD13 and an IC50 value of 1.39 μM for the 20S proteasome. BC-05 can be used in multiple myeloma research.

BTM-3566 is an OMA1 activator. BTM-3566 activates the mitochondrial stress response. BTM-3566 induces apoptosis in diffuse large B-cell lymphomas (DLBCL) cell lines.

Arecaidine hydrobromide, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrobromide is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.

Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine hydrobromide inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.