PI3K

Cat.No. 产品名称 Information

GC32932 Vps34-IN-2 Vps34-IN-2是一种新型的，有效且有选择性的Vps34抑制剂，在Vps34酶促测定和GFP-FYVE细胞测定中的IC50值分别为2和82nM。

GC32916 Parsaclisib (INCB050465)

INCB050465

Parsaclisib (INCB050465, INCB-50465, IBI376) is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.

GC32847 PI4KIIIbeta-IN-9 PI4KIIIbeta-IN-9是一种有效的PI4KIIIβ抑制剂，IC50为7nM。PI4KIIIbeta-IN-9也抑制PI3Kδ和PI3Kγ，IC50分别为152nM和1046nM。

GC32828 Tenalisib (RP6530)

RP6530

Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.

GC32710 GDC-0077 (RG6114)

GDC-0077; RG6114

Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3.

GC31756 IPI-3063 IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5?±?1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher.

GC31751 PI3Kδ-IN-2

YY-20394

PI3Kδ-IN-2 (YY-20394) 是 PI3K&#948 的强效、口服生物利用度和选择性抑制剂；提取自专利WO 2015055071 A1，化合物10； IC50 为 6.4 nM。

GC31666 Seletalisib (UCB5857)

UCB5857

Seletalisib (UCB-5857) is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold).

GC30884 LX2343 An inhibitor of BACE1 and PI3K

GC30156 Brevianamide F (Cyclo(L-Pro-L-Trp))

Cyclo(L-Pro-L-Trp)

An alkaloid with diverse biological activities

GC19471 Leniolisib

CDZ173

An inhibitor of PI3Kδ

GC19411 IITZ-01 IITZ-01 是一种有效的溶酶体自噬抑制剂，具有单剂抗肿瘤活性，对 PI3Kγ 的 IC50 为 2.62 μM。

GC19355 Umbralisib

TGR-1202; RP5264

A PI3K p110δ inhibitor

GC19328 SF2523 A dual inhibitor of PI3K and BRD4

GC19300 PQR309

PQR309

PQR309 是一种有效的脑渗透性口服生物利用度泛 I 类 PI3K/mTOR 抑制剂，对 PI3Kα、PI3Kδ、PI3Kβ、PI3Kγ 和 mTOR 的 IC50 分别为 33nM、451nM、661nM、708nM 和 89nM .PQR309 在人脑胶质瘤细胞中通过抑制增殖、诱导细胞凋亡、诱导 G1 细胞周期停滞、抑制侵袭和迁移等方式发挥抗肿瘤作用。

GC19283 PF-04979064 PF-04979064 是一种有效的选择性 PI3K/mTOR 双激酶抑制剂，对 PI3Kα 和 mTOR 的 Kis 分别为 0.13 nM 和 1.42 nM。

GC19256 MTX-211

Mol 211

MTX-211 (Mol 211) 是 EGFR 和 PI3K 的双重抑制剂，IC50 值 <100 nM。 MTX-211可用于癌症和其他疾病的研究。

GC19202 IPI549

IPI-549

An inhibitor of PI3Kγ

GC19161 GDC-0326 A selective inhibitor of PI3Kα

GC19145 ETP-46321 ETP-46321 是一种有效且具有口服生物利用度的 PI3Kα 和 PI3Kδ 抑制剂，Kiapps 分别为 2.3 和 14.2 nM。

GC19109 CNX-1351 A PI3Kα inhibitor

GC18479 SAR260301

(S)-2-(2-(2-甲基吲哚啉-1-基)-2-氧代乙基)-6-吗啉嘧啶-4(3H)-酮

A selective PI3Kβ inhibitor

GC18164 UCB9608

(S)-4-(6-氨基-1-甲基-1H-吡唑并[3,4-D]嘧啶-4-基)-N-(4-甲氧基-2-甲基苯基)-3-甲基哌嗪-1-甲酰胺

UCB9608 是一种有效、选择性和口服活性的 PI4KIIIβ 抑制剂，IC50 为 11 nM，对 PI3KC2 α、β 和 γ 脂质激酶具有选择性。

GC10228 GDC-0084 PI3K and mTOR inhibitor, brain-permeable

GC15595 GSK2269557 A selective inhibitor of PI3Kδ

GC11910 AS-041164 Selective inhibitor of PI3Kγ

GC12416 INK1117

[6-(2-氨基-5-苯并恶唑基)咪唑并[1,2-A]吡啶-3-基]-4-吗啉基甲酮,MLN1117,TAK-117;Serabelisib

A selective inhibitor of PI3Kα

GC12889 PX 866

PX-866

An inhibitor of PI3K

GC10436 VPS34-IN1

Vacuolar Protein Sorting 34 Inhibitor 1, Vps34 Inhibitor 1

A potent and selective inhibitor of Vps34

GC11248 AZD8835 An inhibitor of PI3Kα and PI3Kδ

GC15679 GSK2292767 A potent and selective inhibitor of PI3Kδ

GC14679 PIK-III

Vacuolar Protein Sorting 34 Inhibitor 2, Vps34-IN2, Vps34 Inhibitor 2

A selective inhibitor of Vps34

GC14371 LY3023414

LY3023414

LY3023414 (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ , PI3Kγ, DNA-PK 和 mTOR, 分别。 LY3023414 在低纳摩尔浓度下有效抑制 mTORC1/2。