potent

CFI-400945 is an potent, selective and orally active inhibitor of polo-like kinase 4(PLK4; Ki value of 0.26 nM).

Ragaglitazar(NNC-61-0029) is a potent dual PPARα and PPARγ agonist that has shown potent lipid-lowering and insulin sensitizing effects in animal models.Ragaglitazar can be used to study type 2 diabetes.

SMCC-DM1 (DM1-SMCC) (DM1-SMCC) is a drug-linker conjugate which composed of a potent microtubule-disrupting agent DM1 and a linker SMCC to make antibody-drug conjugate (ADC).

Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM). Pevonedistat can be used for the treatment of myelodysplastic syndromes (MDS) and also has antitumor activity.

Tirofiban hydrochloride monohydrate (MK-383 Hydrochloride) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist.

AWL-II-38.3 is a highly effective inhibitor of EphA3, a receptor for ephrin-A. It demonstrates potent kinase inhibitory activity against EphA3 and does not show significant cellular activity against Src-family kinases or b-raf [1] [2].

Selitrectinib (LOXO-195) is a potent and selective inhibitor of the receptor tyrosine kinases(TRK)( TrkA and TrkC with IC50s of 0.6 and <2.5 nM, respectively)

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Duvelisib (INK1197) is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities.

ADU-S100 ammonium salt (ML RR-S2 CDA ammonium salt) is an activator of stimulator of interferon genes (STING). ADU-S100 ammonium salt leads to potent and systemic tumor regression and immunity.

MCC950 sodium (CP-456773 sodium) is a potent and selective inhibitor of the inflammatory vesicle NLRP3 (IC50=7.5 nM in BMDMs; IC50=8.1 nM in HMDMs). MCC950 sodium has no effect on other inflammatory vesicles such as AIM2, NLRC4 or NLRP1.

SNDX-5613 is a potent and specific inhibitor of Menin-MLL(Ki of 0.149 nM and a cell based IC50 of 10-20 nM). SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias.

ZN-c3 is a potent and selective Wee1 inhibitor with balanced potency, ADME, and pharmacokinetic properties.

Flovagatran (TGN 255) is an orally active, potent, and selective inhibitor of thrombin and parenteral direct factor II.Flovagatran is used to study venous thromboembolism.

Camonsertib (RP-3500) is a selective, orally active ATR kinase inhibitor (ATRi) with an IC50: 1.00 nM in biochemical assays and exhibits potent antitumour effects. Camonsertib is 30 times more selective for ATR than mTOR (IC50: 120 nM) and is a more active inhibitor of ATM, DNA-PK and PI3Kα kinases. PK and PI3Kα kinases.

Rimegepant (BMS 927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.

PD-1/PD-L1-IN-10 is an orally active PD-1/PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy.

Physalin F is a natural blocker of CaV2.3 (R-type) and CaV2.2 (N-type) voltage-gated calcium channels.It is a secosteroid with potent anti-inflammatory and immunomodulatory activities. Physalin F induces apoptosis of PBMC, decreasing the spontaneous proliferation and cytokine production caused by Human T-lymphotropic virus type 1 (HTLV-1) infection

Ancriviroc(CHEMBL336672), an imidoxime with strong antiretroviral activity, is a potent CCR5 inhibitor that can be used to study HIV.

Futibatinib (FGFR-IN-1) is a novel, potent and highly selective FGFR inhibitor, used for antitumor treatment.

RP-6306 is a potent, selective and orally active PKMYT1 inhibitor (IC50= 14 nM). RP-6306 exhibits a high degree of selectivity for PKMYT1 over other kinases in cellular binding assays. RP-6306 exhibits anticancer effects.

Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48/245 nM). Venetoclax induces autophagy and apoptosis.

BLU-945 is a potent, highly selective, reversible, and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, effective against EGFR with L858R and/or exon 19 deletion mutations, T790M, and C797S mutations. It is utilized in lung cancer research, including non-small cell lung cancer (NSCLC).

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

SR-3306 is a potent and highly inhibitor of brain penetrant JNK.

eCF506 is a potent and selective inhibitor of SRC (IC50 < 0.5 nM)

GSK805 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

Belvarafenib is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.

Navitoclax (ABT-263) is a Bcl-2 inhibitor that binds to Bcl-xL, Bcl-2, and Bcl-w proteins (Ki<1 nM) with potent and oral activity. Navitoclax has antitumor activity and induces apoptosis.

Relamorelin (RM-131), a selective and potent growth hormone-releasing peptide/growth hormone secretagogue receptor (GHSR) agonist, is a potent growth hormone-releasing peptide mimetic with a high affinity for the GHS-1a receptor Relamorelin is a centrally permeable pentapeptide that increases growth hormone levels and accelerates gastric emptying and has potential for studying malignant disease.

ABBV-CLS-484 (Osunprotafib) is a potent PTPN2 inhibitor with subnanomolar activity and antitumor activity that enhances T-cell anti-tumor immunity.ABBV-CLS-484 can be used for the treatment of neoplasms, esophageal cancer, and digestive disorders.

MSA-2 is a potent and orally available non-nucleotide STING agonist.

Y-27632 (Y-27632) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

RBN012759, a potent and selective PARP14 inhibitor, decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.

Cbl-b-IN-3 is a potent proto-oncogene-B (CPL-B) inhibitor of casitas B-series lymphoma (ic50 < 1 nM). Cpl-b, a cyclic E3 ubiquitin protein ligase, is involved in the setting of T lymphocyte activation thresholds. Cpl-b negatively regulates p85 in an independent proteolytic manner, and participates in the recruitment of p85 to CD28 and T cell antigen receptor ζ through its E3 ubiquitin ligase activity. Inhibition of PI3K inhibits the enhancement of Cblb-/ -T cell activation.

Potent, selective agonist of Mu-opioid receptor. Antinociceptive. Stimulates calcium-activated adenylyl cyclases related cAMP production. Expresses chemokines and chemokine receptors through TGF-beta1. Increases food intake of rats.

Aticaprant (LY-2456302) (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).

Caudatin is one of the species of C-21 steroidal glycosides mainly isolated from the root of Cynanchum bungei Decne and exhibits potent anticancer activities.

Lenacapavir (GS-6207) is a potent capsid-targeting inhibitor of HIV replication. Lenacapavir shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells.

VT104 is a potent YAP/TAZ inhibitor with oral activity that can be used in cancer research. VT104 prevents palmitylation of endogenous TEAD1 and TEAD3 proteins.

ADH-503 (GB1275) is a potent agonist of the integrin CD11b to mitigate myeloid cell immunosuppression.

SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SETDB1-TTD with a Kd of 88 nM.

Sunvozertinib (DZD9008) is a potent ErbBs and BTK inhibitor and has inhibitory effects on EGFR, Her2 and mutant epidermal growth factor. Sunvozertinib showed inhibition of EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutation, and Her2 exon 20 YVMA and EGFR WT A431. IC50 were 20.4, 20.4, 1.1, 7.5 and 80.4 nM, respectively.

YKL-05-099 is an inhibitor of the salt-inducible kinase(SIK1 and SIK3 ; IC50s: 10 and 30 nM, respectively). It has a slightly less potent SIK2-inhibitory (IC50:40 nM).

SX-682 is a potent, selective and orally bioavailable inhibitor of CXCR1/2 ,has the potential to treat castration-resistant prostate cancer.

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

BAY-1816032 is a potent and orally available inhibitor of bidding uninhibited by benzimidazoles 1 ( BUB1) kinase (IC50: 7 nM).

Tigemonam is a monobactam. Tigemonam has potent activity against Gram-negative aerobic bacterial pathogens.

Ritlecitinib (PF-06651600) is a potent JAK3-selective inhibitor (IC50: 33.1 nM).