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TMD

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Bacterial (1) Btk (5) Estrogen Receptor/ERR (1) iGluR (1) IRAK (1) mGluR (1) PROTACs (1) Src (1) Wnt (1) γ-secretase (1)
By Research Areas:	Cancer (7) Endocrinology (1) Infection (1) Inflammation/Immunology (2) Neurological Disease (3)

12

Inhibitors & Agonists

1

Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

FSHR agonist 1	Estrogen Receptor/ERR	Endocrinology
FSHR agonist 1 is a high affinity and allosteric follicle stimulating hormone receptor (FSHR) agonist with a pEC₅₀ of 7.72. FSHR agonist 1 formes extensive interactions with the TMD to directly activate FSHR .

GNE-9278	iGluR	Neurological Disease
GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity .

G247	Bacterial	Infection
G247 is a specific MsbA inhibitor. G247 acts as a transmembrane domains (TMDs) wedge, symmetrically increasing nucleotide-binding domains (NBDs) separation and preventing conformational transition of MsbA. G247 suppresses ATPase activity by increasing inter-NBD distance .

UBX-382	Btk	Cancer
UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells .

KIN-8194	Src Btk	Cancer
KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC₅₀ values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice .

HY-119165

GSM-1

γ-secretase Neurological Disease

GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1) .

BTK-IN-27	Btk	Inflammation/Immunology Cancer
BTK-IN-27 (example 8) is a BTK inhibitor (IC₅₀: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC₅₀: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases .

F7H	Wnt	Cancer
F7H is a Frizzled receptor FZD7 antagonist (IC₅₀: 1.25 μM). Frizzled receptors (FZDs) influence Wnt signaling, mediating embryonic development and tissue homeostasis. F7H is a potent ligand for the FZD7 transmembrane domain (TMD) .

IRAK4-IN-16	IRAK	Cancer
IRAK4-IN-16 (compound 4) is a potent IRAK4 (interleukin-1 receptor associated kinase 4) inhibitor, with an IC₅₀ of 2.5 nM. IRAK4-IN-16 shows cytotoxicity activity against OCI-LY10, TMD8, Ramos and HT cells, with IC₅₀ values of 0.2, 0.2, 0.6, and 2.7 μM, respectively .

Ro 67-4853	mGluR	Neurological Disease
Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC₅₀=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .

NX-2127	Btk	Cancer
NX-2127 is an orally and potent BTK inhibitor, inducing degradation of the mutated BTK ^C481S in cells. NX-2127 inhibits proliferation of BTK ^C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells .

NX-5948 BTK-IN-24	Btk PROTACs	Inflammation/Immunology Cancer
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .

Cat. No.	Compare	Product Name	Species	Source

	TTN Protein, Human (His) MPRM; Cardiomyopathy dilated 1G CMD1G; CMH 9; CMH9; CMPD 4; CMPD4; Connectin; HMERF; LGMD2J; MU RMS 40.14; MYLK5; TMD; TTN	Human	E. coli
	The TTN protein is critical for vertebrate striated muscle assembly, establishing microfilament connections that are critical for sarcomeric force balance. TTN coordinates cross-link size and extensibility, shaping sarcomere extensibility and muscle function. TTN Protein, Human (His) is the recombinant human-derived TTN protein, expressed by E. coli , with N-His labeled tag. The total length of TTN Protein, Human (His) is 207 a.a., with molecular weight of ~26.5 kDa.

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