SRD5A1-IN-1 (Compound 4) is a competitive and covalent steroid 5α-reductase type 1 (SRD5A1) inhibitor with an IC50 of 1.44 µM. SRD5A1-IN-1 modulates SRD5A1 function, leading to a lower level of dihydrotestosterone (DHT) production and SRD5A1 protein suppression[1].

CP 226269 is a potent dopamine D4 receptor agonist that induces calcium flux with EC50 of 32.0 nM. CP 226269 can be used in the research of schizophrenia and other related diseases.

ZW290 is a compound to activate brown adipose tissue (BAT) thermogenic function. ZW290 increases the expression of uncoupling Protein 1 (UCP1) protein and inhibits ATP synthesis in BAT.

Methoxyamine is an orally bioavailable small molecule inhibitor with potential adjuvant activity. Methoxyamine covalently binds to apurinic/apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER), which may result in an increase in DNA strand breaks and apoptosis. This agent may potentiate the anti-tumor activity of alkylating agents. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

WAY-639889 is a bioactive compound relative to neuropeptide Y-5.

Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity.

Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes.

SI-2 hydrochloride (EPH 116 hydrochloride) is a highly promising SRC-3 SMI: SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 hydrochloride (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability[1].

MF-094 (MF094) is a potent, highly selective inhibitor of ubiquitin specific protease 30 (USP30) with IC50 of 0.12 uM, demonstrates <30% inhibitory activity for a panel of 22 USPs assays at 10 uM.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.28 uM.

Novel inhibitor of MuRF1, attenuating skeletal muscle atrophy and dysfunction in cardiac cachexia

Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83 μM.

p97-IN-1 is a potent p97 inhibitor with an IC50 <30 nM (WO2015109285A1, compound FF07).

Usp22i-S02(USP22-IN-1, compound S02) is a potent inhibitor of ubiquitin specific peptidase 22 (USP22). It showed anticancer activity by suppressing Foxp3 expression in T-regulatory cells.

Eeyarestatin I is a potent inhibitor of endoplasmic reticulum-associated protein degradation (ERAD). Eeyarestatin I also inhibits Sec61 translocon.

MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer[1][2].

MRT-81 is a potent antagonist of human and rodent smoothened Smo receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer.

M435-1279 is a UBE2T inhibitor. M435-1279 acts inhibit the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.

ALLO-2 is a potent small molecule Smoothened (Smo) antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.

Lirafugratinib (RLY-4008) is an orally active and selective inhibitor of FGFR2.

Cetuximab-MMAE is an antibody-drug conjugate composed of a anti-EGFR monoclonal antibody and a cytotoxic tubulin polymerase inhibitor conjugated through MC-Vc-PAB (maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl) type linker.

Laprituximab emtansine (IMGN-289) is an immunotoxin targeting HER1. Laprituximab emtansine is an EGFR antibody-drug conjugate (ADC) consisting of the J2898A antibody, DM1 (anti-microtubule agent) and the SMCC thioether linker. Laprituximab emtansine can be used for cancer research[1][2][3].

Serclutamab Talirine (ABBV-321), is an antibody-drug conjugate (ADC) composed of an humanized immunoglobulin G1 anti-EGFR monoclonal antibody conjugated to a pyrrolobenzodiazepine (PBD) dimer via a maleimidocaproyl-valine-alanine linker. Serclutamab Talirine has the potential for use in advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR) or its ligands.

JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor. JKE-1674 kills cells in a manner that is equipotent to ML210 and is completely rescued by ferroptosis inhibitors[1].

TMRE is a mitochondria specific dye (λex=550 nm, λem=575 nm).

JNK-IN-7 is a relatively selective JNKs inhibitor(IC50= 1.54/1.99/0.75 for JNK1/2/3); also bound to IRAK1, PIK3C3, PIP5K3 and PIP4K2C.

ASP2453 is a potent, selective and covalent KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.

ERK-IN-3 is a potent and oral of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.

BGB-15025 is a potent and selective HPK1 inhibitor. It is used in the treatment of various cancers.