K252a

K252a
IUPAC名
Methyl (13S,14R,16R)-14-hydroxy-13-methyl-5-oxo-6,7,13,14,15,16-hexahydro-5H-13,16-epoxydiindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocine-14-carboxylate
识别
CAS号 99533-80-9  ☒N
PubChem 3035817
ChemSpider 2299962
IUPHAR配体 336
性质
化学式 C27H21N3O5
摩尔质量 467.47 g·mol−1
溶解性(其它溶剂) 可溶于DMSO二氯甲烷和甲醇
若非注明,所有数据均出自标准状态(25 ℃,100 kPa)下。

K252a是一种分离自拟诺卡氏菌属(学名:Nocardiopsis)细菌的吲哚咔唑类化合物,结构上与星形孢菌素类似[1][2][3][4][5][6][7][8]

参考文献

  1. ^ Ruegg, U.T. et al. (1989) Tips 10, 218.
  2. ^ Eliot, L.H. et al. (1990) B.B.R.C. 171, 148.
  3. ^ Simpson, D.l. et al. (1991) J. Neurosci. Res, 28, 148.
  4. ^ Chin, L.S. et al. (1999) Cancer Invest. 17, 391.
  5. ^ Tapley, P. et al. (1992) Oncogene 7, 371.
  6. ^ Hashimoto, S. (1998) J. Cell Biol. 107, 1531.
  7. ^ Kase, H. et al. (1987) B.B.R.C. 142, 436.
  8. ^ Hirayama E. et al. (2001) B.B.R.C. 285, 1237.

外部連結

  • Wood JL, Stoltz BM, Dietrich HJ. Total synthesis of (+)- and (−)-K252a. J Am Chem Soc. 1995, 117 (41): 10413–4. doi:10.1021/ja00146a039. 
血管生成素英语Angiopoietin receptor
  • 受體激動劑:血管生成素1英语Angiopoietin 1
  • 血管生成素4英语Angiopoietin 4
  • 受體拮抗劑:血管生成素2英语Angiopoietin 2
  • 血管生成素3
  • 激酶抑制劑:Altiratinib
  • CE-245677
  • Rebastinib英语Rebastinib
  • 抗體: Evinacumab英语Evinacumab (against angiopoietin 3)
  • 奈伐库单抗 (against angiopoietin 2)
CNTF英语Ciliary neurotrophic factor receptor
  • 受體激動劑:Axokine英语Axokine
  • CNTF英语Ciliary neurotrophic factor receptor
  • Dapiclermin


 
EGF(ErbB)  
表皮生长因子受体
(EGF(ErbB1/HER1))    
  • 受體激動劑:Amphiregulin英语Amphiregulin
  • Betacellulin英语Betacellulin
  • EGF(尿抑腸素)
  • Epigen英语Epigen
  • Epiregulin英语Epiregulin
  • 人類肝素結合表皮生長因子英语Heparin-binding EGF-like growth factor(HB-EGF)
  • Murodermin英语Murodermin
  • Nepidermin英语Nepidermin
  • 转化生长因子-α(TGFα)
ErbB2/HER2
  • 受體激動劑:Unknown/none
  • 激酶抑制劑:阿法替尼
  • AG-490
  • 拉帕替尼
  • Mubritinib英语Mubritinib
  • Neratinib英语Neratinib
ErbB3/HER3英语HER3
  • 受體激動劑:Neuregulins (heregulins)英语Neuregulin (1英语Neuregulin-1, 2英语NRG2, 6 (neuroglycan C)英语CSPG5)
ErbB4/HER4英语HER4
  • 受體激動劑:Betacellulin英语Betacellulin
  • Epigen英语Epigen
  • Heparin-binding EGF-like growth factor (HB-EGF)英语Heparin-binding EGF-like growth factor
  • Neuregulins (heregulins)英语Neuregulin (1英语Neuregulin-1, 2英语NRG2, 3英语NRG3, 4英语NRG4, 5 (tomoregulin, TMEFF))
FGF
FGFR1英语Fibroblast growth factor receptor 1
  • 受體激動劑:Ersofermin
  • FGF (1英语FGF1, 2 (bFGF)英语FGF2, 3英语FGF3, 4英语FGF4, 5英语FGF5, 6英语FGF6, 8英语FGF8, 10 (KGF2)英语FGF10, 20英语FGF20)
  • Repifermin
  • Trafermin英语Trafermin
  • Velafermin
FGFR2英语Fibroblast growth factor receptor 2
  • 受體激動劑:Ersofermin
  • FGF (1英语FGF1, 2 (bFGF)英语FGF2, 3英语FGF3, 4英语FGF4, 5英语FGF5, 6英语FGF6, 7英语FGF7 (KGF英语keratinocyte growth factor), 8英语FGF8, 9英语FGF9, 10 (KGF2)英语FGF10, 17英语FGF17, 18英语FGF18, 22英语FGF22)
  • Palifermin英语Palifermin
  • Repifermin
  • Sprifermin英语Sprifermin
  • Trafermin英语Trafermin
  • 抗體: Aprutumab
  • Aprutumab ixadotin
FGFR3英语Fibroblast growth factor receptor 3
  • 受體激動劑:Ersofermin
  • FGF (1英语FGF1, 2 (bFGF)英语FGF2, 4英语FGF4, 8英语FGF8, 9英语FGF9, 18英语FGF18, 23英语FGF23)
  • Sprifermin英语Sprifermin
  • Trafermin英语Trafermin
  • 抗體: Burosumab英语Burosumab (against FGF23)
FGFR4英语Fibroblast growth factor receptor 4
  • 受體激動劑:Ersofermin
  • FGF (1英语FGF1, 2 (bFGF)英语FGF2, 4英语FGF4, 6英语FGF6, 8英语FGF8, 9英语FGF9, 19英语FGF19)
  • Trafermin英语Trafermin
Unsorted
  • 受體激動劑:FGF15/19英语FGF15/19
HGF (c-Met)英语Hepatocyte growth factor receptor
  • 受體激動劑:Hepatocyte growth factor英语Hepatocyte growth factor
  • Potentiators: Dihexa (PNB-0408)英语Dihexa
  • 激酶抑制劑:Altiratinib
  • AM7
  • AMG-458
  • Amuvatinib
  • BMS-777607
  • Cabozantinib英语Cabozantinib
  • Crizotinib英语Crizotinib
  • Foretinib英语Foretinib
  • Golvatinib
  • INCB28060
  • JNJ-38877605
  • K252a
  • MK-2461
  • PF-04217903
  • PF-2341066
  • PHA-665752
  • SU-11274
  • Tivantinib英语Tivantinib
  • Volitinib英语Volitinib
IGF英语Somatomedin receptor
IGF-1
  • 受體激動劑:des(1-3)IGF-1英语des(1-3)IGF-1
  • 胰岛素样生长因子1(生長調節素C)
  • IGF-1 LR3英语IGF-1 LR3
  • Insulin-like growth factor-2 (somatomedin A)英语Insulin-like growth factor 2
  • Insulin
  • Mecasermin英语Mecasermin
  • Mecasermin rinfabate英语Mecasermin rinfabate
  • 激酶抑制劑:BMS-754807
  • Linsitinib英语Linsitinib
  • NVP-ADW742
  • NVP-AEW541
  • OSl-906
  • 抗體: AVE-1642
  • Cixutumumab英语Cixutumumab
  • Dalotuzumab英语Dalotuzumab
  • 芬妥木单抗
  • 加尼妥单抗
  • 罗妥木单抗
  • R1507
  • Teprotumumab英语Teprotumumab
  • Xentuzumab (against IGF-1 and IGF-2)
IGF-2英语Insulin-like growth factor 2 receptor
  • 受體激動劑:Insulin-like growth factor-2 (somatomedin A)英语Insulin-like growth factor 2
其他
  • Binding proteins: IGFBP英语Insulin-like growth factor-binding protein (1英语IGFBP1, 2英语IGFBP2, 3英语IGFBP3, 4英语IGFBP4, 5英语IGFBP5, 6英语IGFBP6, 7英语IGFBP7)
  • Cleavage products/derivatives with unknown target: Glypromate (GPE, (1-3)IGF-1)
  • Trofinetide英语Trofinetide
LNGF (p75NTR)英语Low-affinity nerve growth factor receptor
  • 受體激動劑:BDNF
  • BNN-20英语BNN-20
  • BNN-27英语BNN-27
  • Cenegermin英语Cenegermin
  • DHEA
  • DHEA-S英语Dehydroepiandrosterone sulfate
  • NGF英语Nerve growth factor
  • NT-3英语Neurotrophin-3
  • NT-4英语Neurotrophin-4
  • 抗體: 抗NGF: ABT-110 (PG110)
  • ASP-6294
  • 法司努单抗
  • Frunevetmab英语Frunevetmab
  • Fulranumab英语Fulranumab
  • MEDI-578
  • Ranevetmab英语Ranevetmab
  • 他尼珠单抗
  • Aptamers: Against NGF: RBM-004
  • 誘餌受體:LEVI-04 (p75NTR-Fc)
PDGF
  • 受體激動劑:Becaplermin英语Becaplermin
  • PDGFA英语PDGFA, B英语PDGFB, C英语PDGFC, D英语PDGFD
  • 激酶抑制劑:Agerafenib
  • Axitinib英语Axitinib
  • Crenolanib英语Crenolanib
  • 伊马替尼
  • Lenvatinib英语Lenvatinib
  • 马赛替尼
  • Motesanib英语Motesanib
  • 尼達尼布
  • Pazopanib英语Pazopanib
  • Radotinib英语Radotinib
  • Quizartinib英语Quizartinib
  • 舒尼替尼
  • 索拉非尼
  • Toceranib英语Toceranib
  • 抗體: Olaratumab英语Olaratumab
  • Ramucirumab英语Ramucirumab
  • Tovetumab英语Tovetumab
RET (GFL)英语RET proto-oncogene
GFRα1英语GFRα1
  • 受體激動劑:Glial cell line-derived neurotrophic factor (GDNF)英语Glial cell line-derived neurotrophic factor
  • Liatermin
  • 激酶抑制劑:Vandetanib英语Vandetanib
GFRα2英语GFRα2
  • 受體激動劑:Neurturin (NRTN)英语Neurturin
  • 激酶抑制劑:Vandetanib英语Vandetanib
GFRα3英语GFRα3
  • 受體激動劑:Artemin (ARTN)英语Artemin
  • 激酶抑制劑:Vandetanib英语Vandetanib
GFRα4英语GFRα4
  • 受體激動劑:Persephin (PSPN)英语Persephin
  • 激酶抑制劑:Vandetanib英语Vandetanib
Unsorted
  • 激酶抑制劑:Agerafenib
SCF (c-Kit)英语CD117
  • 受體激動劑:Ancestim英语Ancestim
  • Stem cell factor英语Stem cell factor
TGFβ英语Transforming growth factor beta receptor
  • See here英语Template:TGFβ_receptor_superfamily_modulators instead.
Trk
TrkA英语TrkA receptor
  • 受體激動劑:Amitriptyline
  • BNN-20英语BNN-20
  • BNN-27英语BNN-27
  • Cenegermin英语Cenegermin
  • DHEA
  • DHEA-S英语Dehydroepiandrosterone sulfate
  • Gambogic amide
  • NGF英语Nerve growth factor
  • Tavilermide英语Tavilermide
  • Negative allosteric modulators: VM-902A
  • 激酶抑制劑:Altiratinib
  • AZD-6918
  • CE-245677
  • CH-7057288
  • DS-6051
  • Entrectinib英语Entrectinib
  • GZ-389988
  • K252a
  • Larotrectinib英语Larotrectinib
  • Lestaurtinib英语Lestaurtinib
  • Milciclib
  • ONO-4474
  • ONO-5390556
  • PLX-7486
  • Rebastinib英语Rebastinib
  • SNA-120 (pegylated K252a))
  • 抗體: Against TrkA: GBR-900; Against NGF: ABT-110 (PG110)
  • ASP-6294
  • 法司努单抗
  • Frunevetmab英语Frunevetmab
  • Fulranumab英语Fulranumab
  • MEDI-578
  • Ranevetmab英语Ranevetmab
  • Tanezumab英语Tanezumab
  • Aptamers: Against NGF: RBM-004
  • 誘餌受體:ReN-1820 (TrkAd5)
TrkB英语TrkB receptor
  • 受體激動劑:3,7-DHF
  • 3,7,8,2'-THF
  • 4'-DMA-7,8-DHF英语4'-Dimethylamino-7,8-dihydroxyflavone
  • 7,3'-DHF
  • 7,8-DHF英语7,8-Dihydroxyflavone
  • 7,8,2'-THF
  • 7,8,3'-THF英语7,8,3'-Trihydroxyflavone
  • 阿米替林
  • BDNF
  • BNN-20英语BNN-20
  • Deoxygedunin英语Deoxygedunin
  • Deprenyl英语Deprenyl
  • Diosmetin英语Diosmetin
  • DMAQ-B1
  • HIOC英语HIOC
  • LM22A-4英语LM22A-4
  • N-乙酰血清素
  • NT-3英语Neurotrophin-3
  • NT-4英语Neurotrophin-4
  • Norwogonin (5,7,8-THF)英语Norwogonin
  • R7英语R7 (drug)
  • TDP6
  • 受體拮抗劑:ANA-12英语ANA-12
  • Cyclotraxin B英语Cyclotraxin B
  • Gossypetin (3,5,7,8,3',4'-HHF)英语Gossypetin
  • 激酶抑制劑:Altiratinib
  • AZD-6918
  • CE-245677
  • CH-7057288
  • DS-6051
  • Entrectinib英语Entrectinib
  • GZ-389988
  • K252a
  • Larotrectinib英语Larotrectinib
  • Lestaurtinib英语Lestaurtinib
  • ONO-4474
  • ONO-5390556
  • PLX-7486
TrkC英语TrkC receptor
  • 受體激動劑:BNN-20英语BNN-20
  • DHEA
  • NT-3英语Neurotrophin-3
  • 激酶抑制劑:Altiratinib
  • AZD-6918
  • CE-245677
  • CH-7057288
  • DS-6051
  • Entrectinib英语Entrectinib
  • GZ-389988
  • K252a
  • Larotrectinib英语Larotrectinib
  • Lestaurtinib英语Lestaurtinib
  • ONO-4474
  • ONO-5390556
  • PLX-7486
VEGF英语Vascular endothelial growth factor receptor
  • 受體激動劑:Placental growth factor (PGF)英语Placental growth factor
  • Telbermin
  • VEGF (A英语Vascular endothelial growth factor A, B英语Vascular endothelial growth factor B, C英语Vascular endothelial growth factor C, D (FIGF)英语Vascular endothelial growth factor D)
  • Allosteric modulators: Cyclotraxin B英语Cyclotraxin B
  • 激酶抑制劑:Agerafenib
  • Altiratinib
  • Axitinib英语Axitinib
  • Cabozantinib英语Cabozantinib
  • Cediranib英语Cediranib
  • 拉帕替尼
  • Lenvatinib英语Lenvatinib
  • Motesanib英语Motesanib
  • 尼達尼布
  • Pazopanib英语Pazopanib
  • Pegaptanib英语Pegaptanib
  • Rebastinib英语Rebastinib
  • Regorafenib英语Regorafenib
  • Semaxanib英语Semaxanib
  • 索拉非尼
  • 舒尼替尼
  • Toceranib英语Toceranib
  • Tivozanib英语Tivozanib
  • Vandetanib英语Vandetanib
  • WHI-P 154
  • 誘餌受體:Aflibercept英语Aflibercept
其他
  • Additional growth factors: Adrenomedullin英语Adrenomedullin
  • Colony-stimulating factor英语Colony-stimulating factors (see here instead)
  • Connective tissue growth factor (CTGF)英语Connective tissue growth factor
  • Ephrin英语Ephrins (A1英语EFNA1, A2英语EFNA2, A3英语EFNA3, A4英语EFNA4, A5英语EFNA5, B1英语EFNB1, B2英语EFNB2, B3英语EFNB3)
  • 紅血球生成素 (see here instead)
  • 葡萄糖-6-磷酸異構酶(GPI; PGI, PHI, AMF)
  • Glia maturation factor (GMF)英语Glia maturation factor
  • Hepatoma-derived growth factor (HDGF)英语Hepatoma-derived growth factor
  • 白细胞介素/T-cell growth factor英语T-cell growth factors (see here instead)
  • 白血病抑制因子(LIF)
  • Macrophage-stimulating protein (MSP; HLP, HGFLP)英语Macrophage-stimulating protein
  • Midkine (NEGF2)英语Midkine
  • Migration-stimulating factor (MSF; PRG4)英语Migration-stimulating factor
  • Oncomodulin英语Oncomodulin
  • Pituitary adenylate cyclase-activating peptide (PACAP)英语Pituitary adenylate cyclase-activating peptide
  • Pleiotrophin英语Pleiotrophin
  • Renalase英语Renalase
  • 促血小板生成素 (see here instead)
  • Wnt信号通路
  • Additional growth factor receptor modulators: Cerebrolysin英语Cerebrolysin (neurotrophin mixture)
參見
Receptor/signaling modulators
Signaling peptide/protein receptor modulators
Cytokine receptor modulators