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Abc Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (2) Apoptosis (3) Aurora Kinase (1) Autophagy (1) Bacterial (5) BCRP (2) Btk (1) CDK (1) Elastase (1) IRAK (2) MAGL (1) MALT1 (6) P-glycoprotein (2) PDGFR (1) Phosphodiesterase (PDE) (1) SphK (1) Src (1) Trk Receptor (1) VEGFR (1) Wnt (1)
By Research Areas:	Cancer (19) Cardiovascular Disease (3) Infection (5) Inflammation/Immunology (2) Metabolic Disease (1) Neurological Disease (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-125143

ABC34	MAGL	Metabolic Disease
ABC34 is an inactive control compound of JJH260. ABC34 does not inhibit the fluorophosphonate reactivity or fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1. ABC34 can inhibit both ABHD6 and PPT122 .

HY-100950

ABC1183
ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC₅₀ values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities .

HY-122832

ABC99	Wnt	Cancer
ABC99 is an N-hydroxyhydantoin (NHH) carbamate that selectively inhibits the Wnt-deacylating enzyme NOTUM (IC₅₀=13 nM). ABC99 preserves Wnt3A signaling in the presence of NOTUM .

HY-160519

Targocil-II	Bacterial Antibiotic	Infection
Targocil-II (Compound 2) is an ABC transporter inhibitor with a IC₅₀ value of 137 nM. Targocil-II prevents ATP hydrolysis by binding to allosteric sites of the TM domain. Targocil-II has (antibacterial) activity .

HY-145417

G092	Bacterial	Infection
G092 is a potent inhibitor of MsbA. MsbA is an ABC transporter. Transmembrane ATP-binding cassette (ABC) transporters are crucial cellular machines that move molecules small and large across membranes. G092 has the potential for the research of antimicrobial agents .

HY-120252

ABC44	Others	Neurological Disease
ABC44 is a potent serine hydrolase inhibitor with IC₅₀s of 0.1 μM and 6.5 μM for palmitoyl protein thioesterase 1 (PPT1) in situ and in vitro, respectively. ABC44 can be used for researching infantile neuronal ceroid lipofuscinosis .

HY-16015

Opaganib

5+ Cited Publications

Abc294640
SphK Cancer

Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with K_i of 9.8 μM.

Opaganib 5+ Cited Publications Abc294640	SphK	Cancer
Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with K_i of 9.8 μM.

HY-10161

Tozasertib Maximum Cited Publications 12 Publications Verification VX 680; MK-0457	Aurora Kinase Autophagy	Cancer
Tozasertib (VX 680; MK-0457) is an inhibitor of *Aurora A/B/C* kinases with K_i**s of 0.6, 18, 4.6 nM, respectively.

HY-162268

MALT1-IN-13	MALT1 Apoptosis	Inflammation/Immunology Cancer
MALT1-IN-13 (compound 10m) is inhibitor for mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), which to binds MALT1 protease covalently and irreversibly, inhibits MALT1 with the IC₅₀ of 1.7 μM. MALT1-IN-13 inhibits proliferation against ABC-DLBCL and induces apoptosis in ABC-DLBCL HBL1. MALT1-IN-13 regulates mTOR and PI3K-Akt pathways .

HY-121088

Ceefourin 2	Others	Cardiovascular Disease Others
Ceefourin 2 is a potent and highly selective inhibitor of MRP4. Ceefourin 2 inhibits the transport of MRP4 substrates but is not selective for other ABC transporters. Ceefourin 2 shows lower cytotoxicity and higher microsomal and acid stability .

HY-109019

Vorolanib CM082; X-82	VEGFR PDGFR	Cardiovascular Disease Cancer
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895) .

HY-124658

G0507	Bacterial	Infection
G0507, a pyrrolopyrimidinedione compound, is a potent *LolCDE ABC* Transporter** inhibitor. G0507 is a inhibitor of *Escherichia coli* growth and induces the extracytoplasmic σE stress response. G0507 acts as a chemical probe to dissect lipoprotein trafficking in Gram-negative bacteria .

HY-113805

MC70	P-glycoprotein	Cancer
MC70 is a potent and non-selective P-glycoprotein (P-gp) inhibitor with an EC₅₀ of 0.69 µM. MC70 is an ABC transporters inhibitor and anticancer agent. MC70 interacts with ABCB1, ABCG2 and ABCC1 .

HY-126988

SP-Chymostatin B α-MAPI	Elastase	Others
SP-Chymostatin B (α-MAPI) is a strong inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases such as cathepsins A,B,C, H, and L. SP-Chymostatin B weakly inhibits human leucocyte elastase .

HY-15590

AZ-23 3 Publications Verification AZ23; AZ 23	Trk Receptor	Cancer
AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC₅₀s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.

HY-121282

Mepazine 2 Publications Verification Pecazine	MALT1 Apoptosis	Cancer
Mepazine (Pecazine) is a potent and selective MALT1 protease inhibitor with IC₅₀s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis .

HY-121282A

Mepazine hydrochloride 2 Publications Verification Pecazine hydrochloride	MALT1 Apoptosis	Cancer
Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC₅₀s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine hydrochloride affects viability of ABC-DLBCL cells by enhancing apoptosis .

HY-100933

MY-5445	Phosphodiesterase (PDE)	Cardiovascular Disease Inflammation/Immunology Cancer
MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a K_i of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect .

HY-101453

Ceefourin 1
Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma .

HY-111678

ML230 CID44640177; SID 88095709	BCRP	Cancer
ML230 (CID44640177; SID 88095709) is a selective inhibitor of *ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC₅₀*s values of 0.13 μM and 4.65 μM, respectively .

HY-131902

MLT-231	MALT1	Cancer
MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC₅₀ of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC₅₀ of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse .

HY-125176

G907 1 Publications Verification	Bacterial	Infection
G907 is a selective antagonist of ATP-binding cassette (ABC) transporter MsbA with anti-microbial activity. G907 inhibits E. coli MsbA with an IC₅₀ value of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket .

HY-117203A

CDK12-IN-E9	CDK	Cancer
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC₅₀> 1 μM .

HY-160698

SGR-1505	MALT1	Cancer
SGR-1505 is an orally active MALT1 allosteric inhibitor. SGR-1505 inhibits MALT1 enzymatic activity and shows anti-proliferative activity in BTK inhibitor (BTKi)-sensitive and BTKi-resistant activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines. SGR-1505 can be used for research of B-cell lymphomas .

HY-15805

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-130004

MsbA-IN-6	Antibiotic Bacterial	Infection
MsbA-IN-6 is a potent inhibitor of MsbA. MsbA-IN-6 is an antibiotic. Gram-negative ATP-binding cassette (ABC) transporter MsbA, an essential inner membrane protein, transports lipopolysaccharide from the inner leaflet to the periplasmic face of the inner membrane. MsbA-IN-6 kills Escherichia coli through inhibition of its ATPase and transport activity, with no loss of activity against clinical multidrug-resistant strains .

HY-146112

IRAK4-IN-14	IRAK	Cancer
IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC₅₀ of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib .

HY-142648A

(R)-MLT-985	MALT1	Cancer
(R)-MLT-985 (compound 11) is a potent MALT1 protease inhibitor with an IC₅₀ of 3 nM. (R)-MLT-985 has an IC₅₀ of 20 nM for MALT1-dependent IL-2 production in Jurkat cells. (R)-MLT-985 suppresses growth and aberrant CARD11/BCL10/MALT1 complex signaling in ABC-DLBCL cells .

HY-146113

IRAK4-IN-15	IRAK	Cancer
IRAK4-IN-15 (compound 35) is a potent and selective IRAK4 inhibitor with an IC₅₀ of 0.002 µM. IRAK4-IN-15 shows good human PK predictions with low intrinsic clearance. IRAK4-IN-15 shows great synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib. .

HY-155152

P-gp/BCRP-IN-2	P-glycoprotein BCRP	Cancer
P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC₅₀: 1.6 nM) and BCRP (IC₅₀: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells .

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Abc Inhibitors

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