Stem Cell and Derivatives

JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and

M3686 (Compound 29) is a potent and selective TEAD1 inhibitor with an IC50 value of 51 nM. It exhibits weaker binding activity toward TEAD3. M3686 significantly inhibits the cellular activity of YAP-dependent NCI-H226 cell lines, with an IC50 value of 0.06 μM, and demonstrates strong antitumor effects in the NCI-H226 xenograft model.

Lirucitinib is a JAK inhibitor known for its anti-inflammatory properties.

TEAD-IN-1 (Compound 2) is an effective inhibitor of TEAD auto-palmitoylation with an IC50 of 603 nM. It enhances the interaction between TEAD and VGLL4, while diminishing the interaction between YAP and TEAD. TEAD-IN-1 is applicable for cancer research.

JAK2-IN-18 (Compound example1) is a selective JAK2 inhibitor. It effectively inhibits the JAK-STAT signaling pathway, with an IC50 value of less than 100 nM for pSTAT5 in HEL9217 cells. JAK2-IN-18 suppresses the proliferation of abnormally proliferating myeloid cells and is useful in research on myeloproliferative disorders, such as essential thrombocythemia.

(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib is a JAK3 inhibitor(IC50 : 1 nM).

Tyk2-IN-3 is an inhibitor of Tyk2 pseudokinase (IC50: 485 nM).

PF-06263276 selectively inhibits pan-JAK with IC50: JAK1 (2.2 nM), JAK2 (23.1 nM), JAK3 (59.9 nM), TYK2 (29.7 nM).

HDAC6-IN-9 is a γ-secretase modulator that can significantly reduce the level of Aβ42 in mouse brain and can be used to study neurological diseases.

PF-06648671 is a γ-secretase modulator for the treatment of neurodegenerative and/or neurological disorders.

DAPM (gamma-Secretase Inhibitor XVI) is a Notch pathway inhibitor with anticancer activity and antiproliferative effects.

JAK3-IN-18 is a selective and orally active dual inhibitor targeting JAK3 and TEC, with IC50 values of 0.5391 nM and 12.40 nM, respectively. It demonstrates remarkable selectivity for AK1, AK2, and TYK2, with selectivity ratios exceeding 10,000-fold. JAK3-IN-18 exhibits exceptional therapeutic efficacy in a mouse model of experimental autoimmune encephalomyelitis and is applicable for multiple sclerosis research.

TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) with an IC50 of 4.1 μM. It inhibits TGFβ signaling by promoting protein degradation of TGFβ RII. Additionally, TGFβRI-IN-7 can block the transition from endothelial to mesenchymal states and inhibit cell migration, making it useful for cancer research.

Frevecitinibum is a JAK inhibitor targeting JAK1/2/3 and TYK2, suppressing JAK-STAT signaling and used in inflammatory disease studies.

TGFβRI-IN-3 inhibits TGFβR1 with an IC 50 of 0.79 nM with 2000-fold selectivity against MAP4K4.

JDTic, a 4-phenylpiperidine derivative distantly related to analgesics like meperidine and ketobemidone and more closely to the mu opioid antagonist alvimopan, exhibits a notably long duration of action, maintaining effects in animals for weeks following a single dose. This duration is not due to irreversible binding to the kappa opioid receptor but rather to altered activity of c-Jun N-terminal kinases. As a highly selective antagonist for the κ-opioid receptor, without influencing the μ- or δ-opioid receptors, JDTic has shown potential in animal studies for producing antidepressant and anxiolytic effects. It also demonstrates promise in treating addiction to substances such as cocaine and morphine, distinguishing itself structurally from other kappa antagonists like norbinaltorphimine.