dBRD9 dihydrochloride is a potent and selective degrader (PROTAC) of BRD9 with IC50 of 56.6 nM in MOLM-13 cells.dBRD9 is composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide.dBRD9 does not degrade BRD4 or BRD7 at concentrations up to 5 uM.dBRD9 exhibits antiproliferative effects in human AML cell lines.

SD49-7 is an inhibitor of histone lysine-specific demethylase 4 (KDM4) with an IC50 of 0.19 µM.

iJMJD6(WL12) is an inhibitor of arginine demethylase JMJD6 with an IC50 value of 0.22 μM.

JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.

MS023 hydrochloride is a potent, selective and cell-active inhibitor of human type I protein arginine methyltransferases (PRMT), with IC50 values of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.

UZH2 is a potent and selective METTL3 inhibitor with an IC50 value of 5 nM.

A cell-permeable, small-molecule c-Abl kinase activator with pEC50 of 6.1(EC50=794 nM).

Zilovertamab vedotin (VLS-101, MK-2140) is an antibody-drug conjugate (ADC) composed of a humanised monoclonal antibody targeting ROR1 and the anti-mitotic cytotoxic agent monomethyl auristatin E (MMAE). It has potential for the treatment of lymphoid malignancies.

Enapotamab vedotin (EnaV, HuMAX-AXL-ADC) is an AXL-specific human IgG1 antibody conjugated to the microtubule disrupting agent monomethyl auristatin E (MMAE) through a protease cleavable valine-citrulline (vc) linker.

Trastuzumab MMAE is an antibody-drug conjugate (ADC) composed of an anti-HER2 antibody, conjugated to Monomethyl Auristatin E (MMAE), via a Mc linker. Trastuzumab MMAE has the potential for use in research of solid tumors mainly in HER2-positive breast cancer.

Trastuzumab duocarmazine ((vic)-Trastuzumab duocarmazine) is a HER2-targeting ADC that is recognized and cleaved by histone B in tumor cells and selectively targets tumor cells. Trastuzumab duocarmazine has anti-tumor activity and can be used in cancer research related to uterine and ovarian sarcomas[1].

Telisotuzumab vedotin (Teliso-V, ABBV-399) is an antibody-drug conjugate (ADC) composed of the anti–c-Met humanized monoclonal antibody coupled to the cytotoxic monomethyl auristatin E (MMAE) through a mc-val-cit-PABC type linker. Telisotuzumab vedotin can be used for research on advanced solid tumours.

ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN-441958 is highly selective for B1 over B2 receptors, and >500/ 2000-fold selective for the B1 over μ/δ-opioid receptor.IC50 value: 0.26 nM (Ki)Target: B1 Receptorin vitro: ELN-441958 is a novel small molecule bradykinin B1 receptor antagonist, based on the inhibition of agonist-induced increases in intracellular calcium in native and recombinant cells. ELN-441958 does not inhibit the activation of the human bradykinin B2 receptor at concentrations up to 10 μM, showing that it is highly selective for B1 over B2 receptors. ELN-441958 also displays good selectivity for B1 over other receptors examined in a broad screening panel. It is >500-fold and >2000-fold selective for the B1 receptor over the human μ- and δ-opioid receptor, the most potent off-target activity identified. In IMR-90 cells expressing the native human B1 receptor, ELN-441958 produced a concentration-dependent antagonism of the DAKD-induced calcium mobilization with a KB of 0.12 nM. [1]in vivo: ELN-441958 is essentially completely absorbed and produces high plasma levels after oral administration in rhesus monkeys.ELN-441958 has a moderate clearance and volume of distribution in both species following i.v. administration, consistent with the high metabolic stability in rat, rhesus, and human microsomes. ELN-441958 has high oral exposure and moderate plasma half-lives in rats and rhesus monkeys. The oral availability of ELN441958 in rats was 57%. ELN-441958 dose-dependently reduced carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model, with an ED50 3 mg/kg s.c. [1]

Olcegepant(BIBN 4096; BIBN 4096BS) is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor(IC50= 0.03 nM).

Indusatumab vedotin (MLN-0264) is an antibody-drug conjugate (ADC) composed of an anti-human GUCY2C (Guanylate cyclase 2C) monoclonal antibody and a anti-mitotic cytotoxic agent, monomethyl auristatin E (MMAE).

Norepinephrine tartrate is a potent agonist of adrenergic receptor (AR). Norepinephrine activates α1, α2, β1 receptors.

Oleoyl-L-alpha-lysophosphatidic acid sodium salt is an essential metabolite for membrane biosynthesis. LPA interacts with the G protein-coupled receptors (GPCRs), called the LPA receptor and mediates signaling. It acts as a endogenous agonist for LPA1 and LPA2 receptors.

VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.

SMAD3 is a receptor-regulated intracellular protein that functions downstream of TGF-β and activin receptors and mediates their signaling, playing a role in cell proliferation, differentiation, apoptosis and formation of extracellular matrix. Smad3 Inhibitor, SIS3 is a cell-permeable pyrrolopyridine compound that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling with no effect on Smad2, p38 MAPK, ERK, or PI 3-K signaling. It has been shown to reduce TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.

N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively[1]. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[2].

ATM Inhibitor-5 [formula (1)] is a potent inhibitor of serine/threonine protein kinase ATM (extracted from patent WO2022058351A1)[1].

ATR inhibitor 4 (compound 121) is a potent ATR inhibitor. ATR inhibitor 4 has antitumor activity.

5-Ethynyluridine (5-EU) is a potent cell-permeable nucleoside can be used to label newly synthesized RNA. 5-Ethynyluridine can be used for isolation and sequencing of nascent RNA from neuronal populations in vivo. 5-Ethynyluridine can be used to identify changes in transcription in vivo in nervous system disease models.

Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).

ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a Ki value below 1 µΜ[1].

CDK-IN-2 is a potent and sepecific CDK inhibitor.

Debio 0123 (Debio0123) is a potent, orally available, and highly selective Wee1 kinase inhibitor with IC50 of 0.8 nM, Ki of 0.1 nM.Debio 0123 is highly selective to Wee1 on 465 selected kinases in a cellfree system, does not inhibit Plk1 and Plk2, as also reported in recent publications for AZD1775.Debio 0123 exhibits in vitro growth inhibition activity in a broad number of human cancer cell lines (IC50= 0.109 to 7.08 uM).Debio 0123 prevent CDC2 / Cdk1 phosphorylation, induces γH2AX and enhances phosphorylation of histone H3.Debio 0123 induces apoptosis through mitotic catastrophe following cell cycle progression despite accumulation of unrepaired DNA damage both in vitro and in vivo.

CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF.

Stafia-1 is the first STAT5a inhibitor that inhibits STAT5a (IC50=22.2 μM, Ki=10.9 μM) with at least 9‐fold selectivity over STAT5b and higher selectivity against other STAT family members.