SKLB-23bb
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 585025

CAS#: 1815580-06-3

Description: SKLB-23bb, also known as HDAC6-IN-1, is an orally bioavailable HDAC6-selective inhibitor and also has microtubule-disrupting ability.

Chemical Structure

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SKLB-23bb
CAS# 1815580-06-3
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 585025
Name: SKLB-23bb
CAS#: 1815580-06-3
Chemical Formula: C21H24N4O4
Exact Mass: 396.18
Molecular Weight: 396.450
Elemental Analysis: C, 63.62; H, 6.10; N, 14.13; O, 16.14

Price and Availability

Size Price Availability Quantity
1mg USD 450 2 Weeks
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Synonym: SKLB-23bb; SKLB 23bb; SKLB23bb; HDAC6-IN-1;

IUPAC/Chemical Name: Butanamide, N-hydroxy-4-[2-methoxy-5-[methyl(2-methyl-4-quinazolinyl)amino]phenoxy]-

InChi Key: FWXZZFONXWYSEF-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H24N4O4/c1-14-22-17-8-5-4-7-16(17)21(23-14)25(2)15-10-11-18(28-3)19(13-15)29-12-6-9-20(26)24-27/h4-5,7-8,10-11,13,27H,6,9,12H2,1-3H3,(H,24,26)

SMILES Code: O=C(NO)CCCOC1=CC(N(C)C2=C3C=CC=CC3=NC(C)=N2)=CC=C1OC

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: SKLB-23bb is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 17 nM). It is selective for HDAC6 over HDAC1-5 and HDAC7-11 (IC50s = 386->10,000 nM). SKLB-23bb inhibits tubulin acetylation in HeLa cervical cancer cells (EC50 = 58.9 nM) and the proliferation of A375 melanoma and HeLa cells (IC50s = 45 and 49 nM, respectively). It also binds to the colchicine site in β-tubulin and inhibits microtubule formation in MDA-MB-231 cells.
In vitro activity: SKLB-23bb is a potent oral anticancer candidate for selective HDAC6 inhibitor. In vitro, SKLB-23bb presented low nanomolar antiproliferative effects against a panel of cancer cell lines. Western blot analysis confirmed that SKLB-23bb increased acetylation level of α-tubulin. Reference: J Med Chem. 2016 Feb 25;59(4):1455-70. https://pubmed.ncbi.nlm.nih.gov/26443078/
In vivo activity: In solid tumor xenografts, oral administration of SKLB-23bb efficiently inhibited tumor growth, suggesting that SKLB-23bb was an orally bioavailable HDAC6 and microtubule dual targeting agent. Reference: Mol Cancer Ther. 2018 Apr;17(4):763-775. https://pubmed.ncbi.nlm.nih.gov/29610282/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 79.0 199.27
Water 79.0 199.27

Preparing Stock Solutions

The following data is based on the product molecular weight 396.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Yang Z, Wang T, Wang F, Niu T, Liu Z, Chen X, Long C, Tang M, Cao D, Wang X, Xiang W, Yi Y, Ma L, You J, Chen L. Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. J Med Chem. 2016 Feb 25;59(4):1455-70. doi: 10.1021/acs.jmedchem.5b01342. Epub 2015 Oct 13. PMID: 26443078. 2. Wang F, Zheng L, Yi Y, Yang Z, Qiu Q, Wang X, Yan W, Bai P, Yang J, Li D, Pei H, Niu T, Ye H, Nie C, Hu Y, Yang S, Wei Y, Chen L. SKLB-23bb, A HDAC6-Selective Inhibitor, Exhibits Superior and Broad-Spectrum Antitumor Activity via Additionally Targeting Microtubules. Mol Cancer Ther. 2018 Apr;17(4):763-775. doi: 10.1158/1535-7163.MCT-17-0332. PMID: 29610282.
In vitro protocol: 1. Yang Z, Wang T, Wang F, Niu T, Liu Z, Chen X, Long C, Tang M, Cao D, Wang X, Xiang W, Yi Y, Ma L, You J, Chen L. Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. J Med Chem. 2016 Feb 25;59(4):1455-70. doi: 10.1021/acs.jmedchem.5b01342. Epub 2015 Oct 13. PMID: 26443078.
In vivo protocol: 1. Wang F, Zheng L, Yi Y, Yang Z, Qiu Q, Wang X, Yan W, Bai P, Yang J, Li D, Pei H, Niu T, Ye H, Nie C, Hu Y, Yang S, Wei Y, Chen L. SKLB-23bb, A HDAC6-Selective Inhibitor, Exhibits Superior and Broad-Spectrum Antitumor Activity via Additionally Targeting Microtubules. Mol Cancer Ther. 2018 Apr;17(4):763-775. doi: 10.1158/1535-7163.MCT-17-0332. PMID: 29610282.

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[1] Wang F, et al. Mol Cancer Ther. 2018, 17(4):763-775.