TR002 is a novel mitochondrial permeability transition pore (mtPTP) inhibitor.

RO 27-3225 (RO27-3225, RO 273225) is a potent, selective melanocortin melanocortin receptor MC4R agonist with EC50 of 1 nM, >30-fold selectivity over MC3R.

S isomer of BAY-8040.Bay-8040 is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 28 nM; displays no significant inhibition toward 68 other pharmacologically relevant targets (>10 uM), and a panel of related serine proteases; shows in vivo efficacy with regard to decreasing cardiac remodeling and amelioration of cardiac function in monocrotaline-induced rat model for pulmonary arterial hypertension.

SHP504 is a distinct, allosteric site 2 SHP2 inhibitor with IC50 of 21 uM (SHP2 1-525), and selective over the phosphatase domain (SHP2 PTP IC50>100 uM).downregulates DUSP6 mRNA, a downstream MAPK pathway marker, in KYSE-520 cancer cells.

This pool is delivered in subpools of 291 peptides derived from a peptide scan through the entire Spike glycoprotein (Protein ID: P15423) of Human coronavirus 229E (HCoV-229E) for T cell assays. 5mg per peptide, purity>95% Total Length: 1173 AA; Sequence: MFVLLVAYAL LHIAGCQTTN GLNTSYSVCN GCVGYSENVF AVESGGYIPS DFAFNNWFLL TNTSSVVDGV VRSFQPLLLN CLWSVSGLRF TTGFVYFNGT GRGDCKGFSS DVLSDVIRYN LNFEENLRRG TILFKTSYGV VVFYCTNNTL VSGDAHIPFG TVLGNFYCFV NTTIGNETTS AFVGALPKTV REFVISRTGH FYINGYRYFT LGNVEAVNFN VTTAETTDFC TVALASYADV LVNVSQTSIA NIIYCNSVIN RLRCDQLSFD VPDGFYSTSP IQSVELPVSI VSLPVYHKHT FIVLYVDFKP QSGGGKCFNC YPAGVNITLA NFNETKGPLC VDTSHFTTKY VAVYANVGRW SASINTGNCP FSFGKVNNFV KFGSVCFSLK DIPGGCAMPI VANWAYSKYY TIGSLYVSWS DGDGITGVPQ PVEGVSSFMN VTLDKCTKYN IYDVSGVGVI RVSNDTFLNG ITYTSTSGNL LGFKDVTKGT IYSITPCNPP DQLVVYQQAV VGAMLSENFT SYGFSNVVEL PKFFYASNGT YNCTDAVLTY SSFGVCADGS IIAVQPRNVS YDSVSAIVTA NLSIPSNWTT SVQVEYLQIT STPIVVDCST YVCNGNVRCV ELLKQYTSAC KTIEDALRNS ARLESADVSE MLTFDKKAFT LANVSSFGDY NLSSVIPSLP TSGSRVAGRS AIEDILFSKL VTSGLGTVDA DYKKCTKGLS IADLACAQYY NGIMVLPGVA DAERMAMYTG SLIGGIALGG LTSAVSIPFS LAIQARLNYV ALQTDVLQEN QKILAASFNK AMTNIVDAFT GVNDAITQTS QALQTVATAL NKIQDVVNQQ GNSLNHLTSQ LRQNFQAISS SIQAIYDRLD TIQADQQVDR LITGRLAALN VFVSHTLTKY TEVRASRQLA QQKVNECVKS QSKRYGFCGN GTHIFSIVNA APEGLVFLHT VLLPTQYKDV EAWSGLCVDG TNGYVLRQPN LALYKEGNYY RITSRIMFEP RIPTMADFVQ IENCNVTFVN ISRSELQTIV PEYIDVNKTL QELSYKLPNY TVPDLVVEQY NQTILNLTSE ISTLENKSAE LNYTVQKLQT LIDNINSTLV DLKWLNRVET YIKWPWWVWL CISVVLIFVV SMLLLCCCST GCCGFFSCFA SSIRGCCEST KLPYYDVEKI HIQ

STING agonist compound 17 is a selective stimulator of interferon genes (STING) receptor agonist.

MPI_5a is a potent selective inhibitor of HDAC6, and poorly blocks other HDAC enzymes.

LCB-1 is a designed antiviral protein inhibiting SARS-CoV-2. LCB1 is roughly six times more potent on a per mass basis than the most effective monoclonal antibodies reported thus far.LCB1 is currently being evaluated in rodents. LCB1 binds the Spike receptor binding domain (RBD) with affinity below 1 nM and blocks ARS-CoV-2 infection of Vero E6 cells with IC50 of 23.54 pM.

ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRASG12C nucleotide state in living cells.

GSK805, also known as ROR gamma-t-IN-1, is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding.

BIIB068 is a potent, selective, reversible and orally active BTK inhibitor. BIIB068 demonstrated good kinome selectivity with good overall drug-like properties for oral dosing, was well tolerated across preclinical species at pharmacologically relevant doses with good ADME properties, and achieved >90% inhibition of BTK phosphorylation (pBTK) in humans.

A potent inhibitor of sEH (soluble epoxide hydrolase) with IC50 of 18 nM and 69 nM for mouse sEH and human sEH, respectively.

Compound Y-1 exerts the best inhibition activity (IC50 = 0.21 μM) against NA, which is better than oseltamivir carboxylate (OSC) (IC50 = 3.04 μM) and lead AN-329/ 10738021 (IC50 = 1.92 μM).

The (S)-isomer of Viloxazine.

The (S)-isomer of Viloxazine.

BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins.

SALL4 peptide FFW (RRKFAKFQWI, FFW peptide) is a potent therapeutic SALL4 peptide antagonist of SALL4-NURD (nucleosome remodeling deacetylase) interaction with target affinity of 23 nM.

BI-4020 is a highly active, noncovalent EGFR inhibitor against EGFR mutations T790M and C797S with IC50 of 0.6 nM, while shows sparing activity against wild-type EGFR.

Biotin modification of SBP1.SBP1(spike-binding peptide 1) is a first-in-class peptide binder to the SARS-CoV-2 spike protein. SBP1 specifically binds SARS-CoV-2-RBD with low nanomolar affinity. SBP1 to the RBD was determined to be 47 nM with the average Kon = 4.69*104M-1S-1 and Koff=2.2*10-3.The interaction between SBP1 and the RBD of SARS-CoV-2 spike protein was validated by bio-layer interferometry. The KD, derived from protein association and dissociation kinetics, was found to be 47 nM after averaging the fitting values at different protein concentrations. The amino acid sequence of SBP1 is entirely derived from human ACE2 and should be recognized as endogenous by the human immune system. This feature could be highly beneficial in later stages of pre-clinical development.

SIS17 is a potent and selective HDAC 11 inhibitor with an IC50 value of 0.83 μM. SIS17, is active in cells and inhibited the demyristoylation of a known HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.

GAK inhibitor 12r is a higghly potent, selective inhibitor of cyclin G-associated kinase (GAK) with Kd of 89 nM; targets only 8 other kinases with greater than 90% inhibition in a diverse panel of 468 kinases

MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.

Furin inhibitor I is a selective, irreversible, and cell-permeable competitive inhibitor of proprotein convertases, including furin/SPC1 (Ki = ~1 nM), SPC2/PC2 (Ki = 0.36 nM), SPC3/PC1/PC3 (Ki = 2.0 nM), SPC4/PACE4 (Ki = 3.6 nM), SPC6/PC5/PC6, and SPC7/LP

JA2120 (NSC81474) is a potent inhibitor of PARG with IC50 of 25.7 μM.

JA2-3 (NSC29192) is a potent dose-dependent inhibitor of PARG with IC50 of 0.1 mM.

GDC-0575, also known as ARRY-575 and RG7741, is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM. Chk1 inhibitor GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis.

GSK-2807 (GSK 2807, GSK2807) is a potent and selective, SAM-competitive inhibitor of SMYD3 with Ki of 14 nM.

GSK2643943A is a potent USP20 inhibitor with IC50 = 160 nM.

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