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29

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13368	YLF-466D C24	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	YLF-466D (C24) 是一种新型 AMPK 激活剂，可抑制血小板聚集。
T38291	C24 Phytosphingosine (t18:0/24:0)
	C24 Phytosphingosine (t18:0/24:0) is a phytoceramide, which is a family of sphingolipids found in the intestine, kidney, and extracellular spaces of the stratum corneum of the mammalian epidermis. C24 Phytosphingosine (t18:0/24:0) is composed of a phytosphingosine backbone amine-linked to a C24 fatty acid chain. It has been used with other ceramides to create stratum corneum substitutes to study percutaneous penetration and psoriasis in vitro. In a stratum corneum model of healthy skin, the inco...
T35810	C24 dihydro Ceramide (d18:0/24:0) Cer(d18:0/24:0)
	C24 dihydro Ceramide is a sphingolipid that has been found in the stratum corneum of human skin.[1] It is found in higher concentrations in female sebum compared to male sebum.[2] C24 dihydro Ceramide levels positively correlate with cytotoxicity in CCRF-CEM, MOLT-4, COG-LL-317h, and COG-LL-332h T cell acute lymphoblastic leukemia (ALL) cell lines.[4] Levels of C24 dihydro ceramide are increased by 149.49-fold in dihydroceramide desaturase 1 (DEGS1) knockdown UM-SCC-22A human head and neck squam...
T38284	C24 dihydro 1-Deoxyceramide (m18:0/24:0) C24 dihydro 1-Deoxyceramide (m18:0/24:0)
	C24 dihydro 1-Deoxyceramide (m18:0/24:0) is a very long-chain atypical ceramide containing a 1-deoxysphinganine backbone. 1-Deoxysphingolipids are formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 C24 dihydro 1-Deoxyceramide (m18:0/24:0) has been found in mouse embryonic fibroblasts (MEFs) following application of 1-deoxysphinganine alkyne or 1-deoxysphinganine-d3.3 It has also been found in mouse brain, spinal cord, ...
T38283	Tetracosanoyl-sulfatide C24 3'-sulfo Galactosylceramide (d18:1/24:0)
	Tetracosanoyl-sulfatide is an endogenous sulfated glycolipid, which are also known as sulfatides . Tetracosanoyl-sulfatide is the major sulfatide in mature myelin in the central and peripheral nervous systems. Levels of Tetracosanoyl-sulfatide are elevated in plasma derived from patients with metachromatic leukodystrophy, a disorder characterized by arylsulfatase A deficiency, leading to sulfatide accumulation. Unlike C24:1 3'-sulfo galactosylceramide, it does not induce an immune response in mo...
T1845	B-Raf IN 1	Raf	MAPK
	B-Raf IN 1 是选择性B-Raf 抑制剂， IC50为 24 nM。
T10775	c-Fms-IN-2	c-Fms	Tyrosine Kinase/Adaptors
	c-Fms-IN-2 是一种 c-FMS 激酶抑制剂 (IC50 = 24 nM)。
T21448	Abafungin 阿巴芬净,Bay w 6341,UNII-11DI31LWXF	Others	Others
	Abafungin (Bay w 6341) 是抗真菌药物，可抑制由 sterol-C-24-methyltransferase 催化的固醇侧链 C-24位点的甲基转移。
T14363	AZ-23 AZ 23,AZ23	Trk receptor	Tyrosine Kinase/Adaptors
	AZ-23是一种 ATP-竞争性的，口服具有活性的 Trk 激酶 A/B/C 抑制剂，IC50值分别为2 nM (TrkA)，8 nM (TrkB)，24 nM (FGFR1)，52 nM (Flt3)，55 nM (Ret)，84 nM (MuSk)，99 nM (Lck)。
T11125	Durlobactam sodium salt 杜巴坦,ETX2514 sodium salt,杜洛巴坦	Antibacterial	Microbiology/Virology
	Durlobactam sodium salt (ETX2514 sodium salt)是一种 β-内酰胺酶抑制剂，针对 A 类 KPC-2、C 类 AmpC 和 D 类 OXA-24，IC50 值分别为 4 nM、14 nM 和 190 nM。 Durlobactam sodium salt 可用于对包括鲍曼不动杆菌在内的耐药革兰氏阴性菌的研究。
T1415	Gemfibrozil 吉非罗齐,CI-719,Jezil,Decrelip,Lopid	P450; Adrenergic Receptor; PPAR	DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience
	Gemfibrozil (CI-719) 是一种PPAR-α激活剂，可作为降脂药。它也是P450非选择性抑制剂，对 CYP2C9、2C19、2C8 和 1A2 的Ki 值分别为 5.8、24、69 和 82 μM。
T1661	Crizotinib PF-02341066,克唑替尼	c-Met/HGFR; ROS; ALK; Autophagy; ROS Kinase	Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors
	Crizotinib (PF-02341066) 是 c-MET 和 ALK 受体的 ATP 竞争性小分子酪氨酸激酶抑制剂，IC50为 8和20 nM。在细胞的实验中，它抑制 NPM-ALK 的酪氨酸磷酸化和 c-Met 的酪氨酸磷酸化。它也是 ROS1抑制剂。它有肿瘤生长抑制作用。
T3641	NVP-BAW2881 BAW2881	Raf; VEGFR; Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors
	NVP-BAW2881 (BAW2881) 是一种选择性的 VEGFR2抑制剂，其 IC50=9 nM。
T10167	5-Dehydroepisterol	Others	Others
	5-Dehydroepisterol is an episterol derivative with anti-fungal activities. It can be formed by C-5 sterol desaturase and converted into 24-methylenecholesterol by 7-dehydrocholesterol reductase.
T79354	CDK9-IN-24	CDK	Cell Cycle/Checkpoint
	CDK9-IN-24（化合物21a）为高选择性CDK9抑制剂，显著抑止肿瘤生长。该化合物有效抑制细胞增殖，通过降调Mcl-1及c-Myc诱导细胞凋亡，适用于急性髓系白血病研究。
T35979	Benastatin C
	Benastatin C is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2It inhibits glutathione S-transferase (GST; IC50= 24 μg/ml for the rat liver enzyme).2Benastatin C also inhibits the esterase activity of isolated porcine pancreatic lipase (IC50= 10 μg/ml). It increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner. 1.Xu, Z., Schenk, A., and Hertweck, C.Molecul...
T36251	DP-C-4
	DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP[1]. DP-C-4 (1-50 μM; 24 hours) has degradation effects on EGFR and PARP simultaneously in a dose-dependent manner in SW1990 cells[1]. [1]. Mengzhu Zheng, et al. Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP. J Med Chem. 2021 May 26.
T70247	Clemizole sulfate
	Clemizole sulfate is a drug in clinical development for the treatment of hepatitis C virus (HCV) infection. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole is an H1 antagonist. Clemizole, an antihistamine drug that was once widely used for treatment of allergic disease, was recently discovered to be a potent inhibitor (IC50, 24 nM) of the interaction between an HCV protein (NS4B) and HCV RNA. Although clemizole was widely used during the 1950s and 1960s, this was before contemporary ...
T37798	Petromyzonol
	Petromyzonol is a tetrahydroxy stearol which serves as the primary spawning pheromone in adult sea lamprey. It is produced in the bile of sea lamprey larvae from the bile acid precursor allocholic acid. While the adult sea lamprey is relatively insensitive to petromyzonol itself, the C-24 sulfate ester (petromyzonol sulfate) is a pheromone and a spawning chemoattractant which can be detected at very low concentrations by lamprey olfactory chemoreceptors. Petromyzonol, petromyzonol sulfate, and a...
T36766	Palmitoylcholine (chloride)
	Palmitoylcholine is an acyl choline.1It inhibits protein kinase C activity when used at a concentration of 100 μM.2Palmitoylcholine induces hemolysis in rat erythrocytes.3Plasma levels of palmitoylcholine are decreased in female patients with myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS).1 1.Germain, A., Barupal, D.K., Levine, S.M., et al.Comprehensive circulatory metabolomics in ME/CFS reveals disrupted metabolism of acyl lipids and steroidsMetabolites10(1)34(2020) 2.Nakadate, T.,...
T69200	CGP74514A
	CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and...
T35533	6-Hydroxypyridin-3-ylboronic Acid
	6-Hydroxypyridin-3-ylboronic acid is a heterocyclic building block.1,2It has been used in the synthesis of non-nucleoside inhibitors of hepatitis C virus (HCV) RNA-dependent RNA polymerase nonstructural protein 5B (NS5B).16-Hydroxypyridin-3-ylboronic acid has also been used in the synthesis of mammalian target of rapamycin (mTOR) inhibitors.2 1.Hendricks, R.T., Spencer, S.R., Blake, J.F., et al.3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymeraseBioorg. Med. Chem. Lett.1...
T14072	A-443654	ERK; VEGFR; GSK-3; FLT; Casein Kinase; MAPK; Akt; PKA; Chk; CDK; Src; PKC; S6 Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	A-443654 是 pan-Akt 抑制剂，对Akt1，Akt2，和Akt3具有同等效力的抑制作用，Ki=均为 160 pM。
T35829	CC-90005
	CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS...
T36668	Geranylgeranoic Acid
	Geranylgeranoic acid (GGA) is an isoprenoid that has been found inS. chinensisand has anticancer activity.1It induces apoptosis in Huh7 and PLC/PRF/5 human hepatoma cells and MLE-10 transformed mouse hepatocytes, but not primary mouse hepatocytes, when used at concentrations ranging from 1 to 20 μM. GGA (10 μM) induces apoptosis in Huh7 cellsvialoss of the mitochondrial membrane potential and activation of interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32).2It also...
T38297	Ribavirin-13C5 Ribavirin-13C5
	Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coro...
T35582	H-Arg-Gly-Asp-Cys-OH (trifluoroacetate salt)
	H-Arg-Gly-Asp-Cys-OH is a tetrapeptide that contains the arginine-glycine-aspartate (RGD) motif, a sequence that acts as a recognition site for various adhesion proteins.1It inhibits the binding of fibrinogen to endothelial cells and ADP-stimulated platelets with IC50values of 320 and 35 μM, respectively.2Implantation of titanium rods coated with H-Arg-Gly-Asp-Cys-OH increases bone formation in rat femurs.3H-Arg-Gly-Asp-Cys-OH has been conjugated to polyethylenimine to improve gene transfection ...
T37594	Pericosine A
	Pericosine A is a fungal metabolite that has been found inP. byssoidesand has anticancer activity.1It inhibits the growth of a variety of cancer cells, including breast, colon, lung, ovary, stomach, and prostate cell lines (GI50s = 0.05-24.55 μM) and increases survival in a P388 mouse xenograft model when administered at a dose of 25 mg/kg. Pericosine A inhibits EGFR by 40 to 70% when used at a concentration of 100 μg/ml. It also reacts with organosulfur compounds in skunk spray to form stable t...
T37187	D-erythro/L-threo Lysosphingomyelin (d18:1) D-erythro/L-threo Lysosphingomyelin (d18:1)
	Lysosphingomyelin is an endogenous bioactive sphingolipid and a constituent of lipoproteins.1,2It is produced by the removal of the acyl group from sphingomyelin by a deacylase and acts as a precursor in the biosynthesis of sphingosine-1-phosphate . D-erythroLysosphingomyelin is an agonist of the S1P receptors S1P1, S1P2, and S1P3(EC50s = 167.7, 368.1, and 482.6 nM, respectively, for the human receptors).3It is also an agonist of the orphan receptor ovarian cancer G protein-coupled receptor 1 (O...

化合物

Cat.No: T13368

Synonym: C24

Target: AMPK

C24 Phytosphingosine (t18:0/24:0)

Cat.No: T38291

C24 dihydro Ceramide (d18:0/24:0)

Cat.No: T35810

Synonym: Cer(d18:0/24:0)

C24 dihydro 1-Deoxyceramide (m18:0/24:0)

Cat.No: T38284

Synonym: C24 dihydro 1-Deoxyceramide (m18:0/24:0)

Tetracosanoyl-sulfatide

Cat.No: T38283

Synonym: C24 3'-sulfo Galactosylceramide (d18:1/24:0)

Cat.No: T1845

Target: Raf

Cat.No: T10775

Target: c-Fms

Cat.No: T21448

Synonym: 阿巴芬净,Bay w 6341,UNII-11DI31LWXF

Target: Others

Cat.No: T14363

Synonym: AZ 23,AZ23

Target: Trk receptor

Durlobactam sodium salt

Cat.No: T11125

Synonym: 杜巴坦,ETX2514 sodium salt,杜洛巴坦

Target: Antibacterial

Cat.No: T1415

Synonym: 吉非罗齐,CI-719,Jezil,Decrelip,Lopid

Target: P450, Adrenergic Receptor, PPAR

Cat.No: T1661

Synonym: PF-02341066,克唑替尼

Target: c-Met/HGFR, ROS, ALK, Autophagy, ROS Kinase

Cat.No: T3641

Synonym: BAW2881

Target: Raf, VEGFR, Bcr-Abl

5-Dehydroepisterol

Cat.No: T10167

Target: Others

Cat.No: T79354

Target: CDK

Cat.No: T35979

Cat.No: T36251

Clemizole sulfate

Cat.No: T70247

Cat.No: T37798

Palmitoylcholine (chloride)

Cat.No: T36766

Cat.No: T69200

6-Hydroxypyridin-3-ylboronic Acid

Cat.No: T35533

Cat.No: T14072

Target: ERK, VEGFR, GSK-3, FLT, Casein Kinase, MAPK, Akt, PKA, Chk, CDK, Src, PKC, S6 Kinase

Cat.No: T35829

Geranylgeranoic Acid

Cat.No: T36668

Cat.No: T38297

Synonym: Ribavirin-13C5

H-Arg-Gly-Asp-Cys-OH (trifluoroacetate salt)

Cat.No: T35582

Cat.No: T37594

D-erythro/L-threo Lysosphingomyelin (d18:1)

Cat.No: T37187

Synonym: D-erythro/L-threo Lysosphingomyelin (d18:1)

Cat. No.	Product Name	Target	Signaling Pathways
T38285	C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z)) C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))	Others	Others
	C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))是成熟髓鞘中主要的硫酸盐类化合物。C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z)) 在大鼠小脑中发现活跃的髓发生鞘化反应时积累率高于C24 3'-sulfo 半乳糖甘油酰胺。C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))与C 型凝集素和免疫球蛋白样受体相互作用使对LMIR5的亲和力高。C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))诱导嗜碱细胞产生MCP-1，可通过增加LMIR5激活NFAT，但不能诱导肥大细胞。C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))在体外与CD1d 结合，并增加游离小鼠脾细胞的增殖。
T5234	Glycoursodeoxycholic acid Ursodeoxycholylglycine,甘氨熊胆酸,GUDCA	Others; Endogenous Metabolite	Metabolism; Others
	Glycoursodeoxycholic acid (Ursodeoxycholylglycine) 是一种酰基甘氨酸和胆汁酸-甘氨酸缀合物，是熊去氧胆酸的代谢物。
T36961	Malformin C
	Malformin C is a natural fungus-derived bicyclic pentapeptide that has antibacterial properties, particularly against species of Bacillus. Malformin C potently blocks the ability of bleomycin to induce G2 arrest in human T-cell leukemia-derived Jurkat cells (IC50 = 0.9 nM). It less potently abrogates colchicine-induced M phase arrest in Jurkat cells (IC50 = 24 nM). Malformin C inhibits cell growth dose-dependently in Colon 38 and HCT 115 cancer cells (IC50s = 0.27 and 0.18 μM, respectively) but ...

天然产物

C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))

Cat.No: T38285

Synonym: C24:1 3'-sulfo Galactosylceramide (d18:1/24:1(15Z))

Target: Others

Glycoursodeoxycholic acid

Cat.No: T5234

Synonym: Ursodeoxycholylglycine,甘氨熊胆酸,GUDCA

Target: Others, Endogenous Metabolite

Cat.No: T36961

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